This invention relates to compounds which have inhibitory effect or blocking effects on substrates (for example, lipids, carbohydrates, amino acids) of less than 10000 of molecular weight which has constituted structure and function of organism fundamentally and, function which is generated by macromolecules such as peptides, proteins, enzymes, nucleic acids and genes (DNA, tRNA, mRNA, rRNA) which are synthesized biologically. These applications of those inhibitory effects or blocking effects relate to antibacterial agents, antifungal agent, antiviral agent, bactericidal and/or sterilized agents (food stuff preserving agents, germination inhibitory or maturation inhibitory agents for fruits and vegetables, antibacterial agents accompanied with forming or elaborating process of plastics, antimicrobial coating materials and, waxes for interior materials and floor, preventable agents of bacterial and fungal proliferation and/or infection for house holding electric instruments, daily use goods, house furnishings and, agents for preventing of bacterial and fungal proliferation and/or infection for paper and pulp such as slime cleaning agents on industrial field of electronics, preventable agents of bacterial and fungal proliferation and/or infection for metal processing, preventable agents of bacterial and fungal proliferation and/or infection for the disposal of wastes), and those are also related to anticancer drugs, contraceptive agents for external use and/or spermatocidal agents, anticoagulants and/or antifibrinolytic agents, modulating agents of function of bioactive substances and/or inhibitors of bioactive substances such as enzymes, peptides, genes and so on, inhibitory and/or blocking agents of antigen-antibody reaction, organ and tissue preservatives, thrombolytic agents, conformation altering agents of saccharide-chains, agents for preventing arteriosclerosis, metabolism (lipids, sugar) improving agents, agents for wound healing, epithelialization promoting agents (including restoration effect of hair). Moreover, those are related to reductants of non-biological molecules (phospholipids, glyceryl group, sulfudoryl group, thiol ester group, monosaccharide and disaccharide with polysaccharide, silicone, vinyl, cellulose and so on), free radical scavengers, desulfurization agents and/or oxidation preventing agents. In addition, those are related to the following effects concerning low molecules and/or macromolecules of non-biological substances, based on chemical and orbital dynamic concept concerning the inhibitory or blocking agents of molecular generating and/or inducing functions, which is proposed in this invention. Those are related to depolymerization agents, improving agents for surface active substances, phase transition agents, improving agents of phase transition, plasticity and/or elasticity promoting agents, plasticity and/or elasticity improving agents (plasticizers), fiber flexibility promoters, improving agents for fiber flexibility, glutinous agents, viscidity improving agents, adhesives, adhesive property improving agents, painting agents, improving agents of painting, moldability improving agents, improving agents of molding forming and/or fabrication, copolymerization agents, stabilizers, antioxidants, improving agents for filling and plugging, agents for improving smoothness, ultraviolet rays absorbents, ultraviolet rays absorptivity improving agents, shock-resistant improving agents, improving agents for light stability, improving agents of mold lubricants, mold releasing agents, parting agents or surface lubricants, improving agents of molecular ring creator. Moreover, those are related to improving agents of wear resistance and/or abrasion resistance, aging resistors and/or durability, improving agents of material property and it""s function, fluidability improving agents, improving agents for property of water absorption, improving agents for property of water resistance, improving agents for rigidness, hardness and softness, improving agents of crystallized materials and/or amorphous materials, flexibility promoters, and improving agents for changing flexibility. And, those are related to improving agents of physical property of macromolecules composite materials, function improving agents of macromolecules composite materials, improving agents of physical property of functional macromolecules composite materials, function improving agents of functional macromolecules composite materials, modulation agents and/or improving agents of excitation wavelength and fluorescent wavelength on pigmentums, coating materials, cosmetic pigments, colorants, photolysis agents and improving agents of photolysis.
Formerly, it has been well known that the basic principle of organic structural chemistry such as bond angle, molecular weight, acidity, bond length, structure, hydrogen bond, resonance, basicity, optical activity, configuration, and conformation is important as well as mechanism of chemical reactions (by Morrison and Boyd, organic chemistry, 6th edition, Tokyo Kagaku Doujinn publication at reference  less than ref. 1 greater than ). On the other hand, for example, elements of living organism consist of lipids, carbohydrates, proteins, enzymes, nucleic acids, macromolecules amino acids and peptides and genes (for example, DNA, tRNA, mRNA, rRNA) and by those elements, in addition, formation of cell membrane, intracellular organella, intracellular and/or extracellular substrates are constructed. Function of these complex substances is generated by multi-dimensional structure (conformation) depending on each substance. In order to understand the mechanism which is related to development and generation of each physiological function (recognition and/or acceptance of substance), it is important to understand the multi-dimensional structure which each substance has. (Alberts, Bray, Lewis, Raff, Roberts and Watson works, The Molecular Biology of the CELL, Garland Publishing Inc., 3th. edition  less than ref. 2 greater than ). It is also known that methyl group contributes in order to produce fluidability and hydrophobicity of substances in the non-living organism, which contains lipids, proteins and so on.  less than ref. 1 greater than . The cell membrane of organism, which is the base units separating from external environment, also consists of hydrophobic component of lipids outside a membrane. And, this cell membrane has important role in signal acceptance into a cell from another cell. To connect and adhere between each cell and to surround intercellular organella also constructed with extremely thin film-like membrane which consist of lipids and proteins molecules. The proteins which is embedded in the membrane has highly biological activities as intermediates around the cell, and between an inside of organella and cytoplasm. According to types of cells, it is an existence of various enzymes which involves in intracellular signal transduction and in intercellular respiration. In addition, it is also known that there is a substance such as tubulin which is relation on morphologic keep of cell, mitosis and prolifelation. Moreover, proteins in a plasma membrane contribute to recognize signals between cells. Hydroxyl group, sulfudoryl group (xe2x80x94SH) and disulfide bond are constituted ester. According to these cross-linking reaction, also, physiological functions which are generated by multi-dimensional structure of a substance are altered. In addition, amino nitrogen generates property of basicity as well as nucleophilic property on molecular reaction. When peptides and proteins are denaturated, coiling of each peptide and proteins is relaxed. Thus, the particular multi-dimensional structure of the peptide and proteins is crumbled, followed by losing a particular bioactivity of the peptides and proteins. Moreover, such change in conformation appears not only in peptide and proteins but in complex substance with phospholipids and glycoproteins (for example, nucleic acids). In addition, in order to maintain a specificity of each physiological function which is generated by moiety of membrane, a substance which is secreted into the outside of cells, enzymes which exists into the cell, cytoskeleton and a substrate which is synthesized within cell, it is also known that it is important that each substance forming living organism has two-dimensional and three-dimensional configuration such as helical structure and sheet. A state of charge distribution and electric charge density of molecules which consist of substances and is generated function by these multi-dimensional structure differs in species differences and morbidity  less than ref. 2 greater than . In addition, virus, which has not cell membrane and is not living organism, consists of peptides chain which are constructed by many amino acid bindings. And, these virus particles have also multi-dimensional structure such as two-dimension and/or three-dimension. Among multi-dimensional structure, helical structure is formed in 3.6 amino acid residues per one helical rotation. Thus, it produces a space which side chain can occupy. And, possible hydrogen bonds on this helical structure can be constituted all. In addition, multi-dimensional structure generates the function of xcex1 domain, beta domain, xcex1/beta domain, exon or intron. This concept is also a scientific fact and important knowledge. Though a core part of this structure is conserved in homologous proteins, dimensional changes in a helix loop region occur. Moreover, formation of conformation depends on a type of the secondary structure to bind each loop and a number of amino acids in helix loop rather than amino acid sequences. Therefore, it is in general to be determined by combination of xcex1-xcex1, betaxe2x80x94beta, xcex1-beta or beta sheet-xcex1 loop. And, multi-dimensional structure of helix loop induces a change of cytoskeleton, mitosis and prolifelation according to change in conformation of each substance (for example, tubulin and spectrin) resulting from changes in an intracellular energy. Moreover, recent scientific topics is to know mechanism of oncogeneis, mechanism of anticancer agents, mechanism of anti-proliferation, natural cell death (for example apoptosis), mechanism of aging process of the nerve cell, cell recognition or mechanism of cell adhesion. While such scientific knowledge is turned into basement, it is hoped for development of new drugs which is utilized to organism such as human being. Though pharmacological effects of conventional antibacterial agents and anticancer drugs have been introduced at cell death, primary mechanism of cell death due to those conventional antibacterial agents and anticancer drugs is to raise denaturation, coagulation and/or necrosis. For this reason, an appearance of mutants and resistant strains as major scientific problems has been left numerously to be resolved. From such a reason, additionally, scientific interest in mechanism of apoptosis arises at present. Moreover, living organism can move automatically by a flagellum and pilli, and a supermicro-size of motor has been provided for pilli of spermatozoa. On driving motor of this organism, energy which is generated by hydrolysis of ATP is utilized. A change in this energy produces to alter multi-dimensional structure of the helix loop which is configurated by myosin. These multi-dimensional structure is to apply to molecular biology of every kinds of genes and antibodies from recent knowledge. It is well known scientific fact and knowledge that it is important to generate physiological function based on recognizing two- or three-dimensional conformation of each substance  less than ref. 2 greater than . But, it has been known that the substance which consists of living organism does not usually exist in an initial position and, it exists in dynamic state (for example, movement of membrane proteins is slower than that of lipids molecules which is about 100 times later). In addition, if movement of lipids molecule results in more animation, fluidability of a membrane indeed becomes larger. But, the speed of the movement differs dependently on types of lipids. A self-action adjustment capability of membrane fluidability holds in organism. On the other hand, it is also known that a hindrance of those adjustment capability causes onset of diseases in human being. For this reason, it is hoped standby that the countermeasure is proposed against a hindrance of the adjustment capability. In addition, interaction of hydrophobicity between hydrophobic groups is greatly committing in stability of lipids bilayer of the biomembrane which is known as a fluidability model. Moreover, since side chain of many amino acids with hydrophobic property flanking in an inside of proteins, it does not come in contact with to water. For this reason, it is also well known that multi-dimensional structure of proteins is kept by hydrogen bond, hydrophobic interaction and van der Waals force and, it makes a flexible matrix. Greater hydrophobic solute is more easily to bind to proteins. In order to get in a hydrophobic region close at proteins surface which hydrophobic molecule exists, it is thought that conformation of proteins changes. In this way, when life events is understood, it is to be important to understand life activity dynamically and multidimensionally. According to a base of the scientific logic mentioned above, the scientific interest in controlling quality of physiological activity is needless to say and, proposal of a new manner for prevention and treatment of various kinds of diseases is eagerness historically.
Though it is not necessary to do more than to read history of relationship between a man and diseases, a fighting to pathogenic microbacterial infection such as bacteria and virus, it is serious problems which needs a medical resolution. And, even though development of advanced medical technology, it is a serious problem that multiple organ failure accompanied with sepsis and disseminated intravascular coagulation causes to result in the death of human being (Hypotensionxe2x80x94for clinician to understanding pathophysiologyxe2x80x94Fujita Publ. by Koyama)  less than ref. 3 greater than . Various kinds of pathogenic microbacteria such as staphylococcus aureus, streptococcus, E. Coli, acid-fast bacteria, mycete and virus usually exist on the living space of human being as origin of various infectious diseases. Up to this time, sanitatory administration to the living space of human being can have been turned into prevention of this pathogenic microbacterial and viral infection. Thus, lots of drugs are utilized in a treatment and prevention for infectious disease in living space of human being, by using disinfectant and/or bactericidal agents. As a result, lots of the fruits have been raised. However, while development of antibacterial agents is noticeable, application of drugs concurs at an appearance of a resistant strain and, a social administrative problem as well as difficulties of medical care has been raised. For example, it is an appearance of various kinds of multi-drug resistant strains which represent methitilin resistance staphylococcus aureus ( less than MRSA greater than  with abbreviation). In order to show resistance to lots of beta-lactam group drugs in staphylococcus aureus, a treatment for infectious disease due to MRSA is difficult and, it becomes pathogenic organism such as opportunistic infection and postoperative infection in clinical practices and, an infected patient to this MRSA changes a serious illness and, he is easy to fall into sepsis and multiple organ failure. Thus, onset of untreatable infection due to MRSA is a serious social issue. An infection of pseudomonas aeruginosa is anxious for preventing secondary infection from burn injury as a complication. From a point of related view with cystic pulmonary fibrosis, recently, an approach to preventing this infection of pseudomonas aeruginosa is a great problem. Moreover, many interests are recently brought nearer to helicobacter pylori as a cause of peptic ulcer or abhorrent factor. In addition, infection of acid-fast bacteria and mycete is international problems as for an infectious complication whose acquired immune deficient syndrome (AIDS) is fatal. Therefore, it is an important international request that it is developed valid drugs on an infectious disease by virus, drugs which have potencies of antimicrobacterial effect to MRSA and/or acid-fast bacteria, drugs for E. Coli which is easy to cause sepsis, drugs which have potencies of antifungal effect.
And also, recently, opportunistic infection in daily living space (for example, air-conditioning contamination according to regionerae) and on surrounding in life behavior as well as in a hospital become serious problems and, bactericidal and/or sterilized agents is recognized again as a prevention countermeasure of bacteria contamination including opportunistic infection. An appearance of society which is populated by many aged generation has been appealed in the near future and, urgent technological development is expected a counterattack of medical care for the aged.
Generally, staphylococcus aureus, acid-fast bacteria, mycete and virus are easy to encounter an opportunity of an infection through respiratory system such as nasal cavity and pharynx, and through digestive tract. Conventional bactericidal and/or sterilized agents frequently depends on a physical manner by living space of human being and at surroundings in life behavior and, moreover, major administration route of drugs such as antibiotic is sometimes restricted in the way of oral administration, intravenous administration and/or direct administration to the infection focus and, there is some apprehensions and inconveniences to medical care specialists, a nursing volunteers and home helpers as well as patients them self. But, during a period which people is alive, we have to continue to come in contact with an external air through skin and respiratory system. Thus, it is expected to utilize room air which is living space for preventing or treating infectious diseases. Generally, in order that bacteria can obtain their resistant abilities by various genetic mechanism such as mutation, selection, character introduction, autotransduction of plasmid, bacterial infection can not be prevented completely by using of conventional simple substance which is chemically synthesized and, the chemotherapeutic agents without induction of being a resistant strain also have not supplied until the present. And, as an aim for an inhibition of a primary structure of the substances which consist of bacterial membrane, a few of drugs with antimicrobacterial effect has been applied abundantly. All the more, while developments of an administration manner of antibacterial agents are also important and are anticipated, additional development of new antibacterial, antifungal agents and/or and antiviral agents which affect on multi-dimensional structure is expected strongly. Moreover, for a marked increase in population on the earth, namely developing countries, it is important to propose a possible planning of birth control even in regarding with supplying foods and trusting of natural resource in the future. However, though a use of physical contraception such as condom and pessary is as a matter of course as for planning of birth control, ovulation control by use of a female sex hormone and operative contraception to both male and female is driven proposal internationally. In order to avoid to be damaged the heredity information of spermatozoa to suppress it""s fertility, a new method of the contraception which can inhibit a movement ability of spermatozoa is also expected. On the other hand, in order to generate the function of living organism, multi-dimensional structure of substances as above-mentioned plays an important role. However, though it is expected that a substance with simple chemical structure can inhibit and/or block the function generated or induced by the multi-dimensional structure of biological substances, there is not proposal of such representative substance, which is little harm and safety, concerning life continuation as integrated whole body at the present. Not only proposal of such representative substances and several proofed efficiencies above mentioned is interest in academic events such as biology, chemistry and medicine, but it is sought that such a suggestion is hastily proposal in practical medical care.
Numerous daily materials, industrial and environmental materials are provided to develop at the present society by understanding, analyzing, manufacturing and improving physical property of low molecule substances and macromolecules substances and by utilizing their functional properties. But, by qualitatively advancing improvement of physical property of low molecule substances and macromolecules substances, an expectation is to propose a representative which makes function, efficiency, comfortableness and safety. For example, physical property of a macromolecules substance such as surface activity substance and polymerization substance is described briefly.
A magnitude of surface activity relates on criticality density for micell formation and solubilization. And, Krafft point is lower as a chain-like (rod-like) part with the substance is short. It is known that a value of criticality density of micell formation is greater as a chain-like (rod-like) part with the substance is short. According to each characteristic configuration of molecule in surface-active agents and/or surfactants, it can effectively produces bubbling formation, wetting, a fall of surface tension, emulsification (formation of emulsion), solubilization, formation of micelle detergency. In addition, in a case of substance with properties of water insoluble and strong hydrophilic, a less intermolecular force between it""s molecule and broad wide spreading on the water surface, it is also known that a membrane with one molecular layer (single molecular film) is formed. If this single molecular film can be transferred on the surface of solid, a surface of hydrophobicity is obtained. For this reason, proposal of improving agents for surface active substances is that it is prospected in making thin film such as LB membrane. In addition, surface-active agents and/or surfactants has a potency of disinfection, stability in hard water. By utilizing these effect, surface-active agents and/or surfactants are blended cosmetics, cleansing creams, shampoos and rinses and, they are widely utilized in electrically charging preventive agents (antistatic agents) of plastics and fibers, softening agents of fibers, foaming, frothing, lathering or whipping agents of aerosol and tinction assistants. Thus, proposal of improving agents for surface active substances is prospected in many fields. Moreover, polyethylene is representative in various kinds of polymers. Polyethylene is a thermoplastic crystal which is repeated of xe2x80x94CH2CH2xe2x80x94 and, it produces branches dependently on a manufacturing method resulting in decrease in crystallinity and rigidity as well as increase in transparence. In addition, polyethylene is added short chained branch (for example, ethyl branch and butyl branch) by pull out reaction (abstraction reaction) of hydrogen within molecule due to back-biting during polymerization resulting in low density and, branch (long chained branch) which is identical to main chain of the polymer is produced by pull out reaction (abstraction reaction) of hydrogen between molecules. Linear polyethylene (LLD polyethylene) has an intensity for impact force. In addition, medium density polyethylene (MD polyethylene) and ultra-low density polyethylene (VLD polyethylene) are used as improving or reforming agents of resins. Ultrahigh molecule weight polyethylene (UHMW polyethylene) is applied widely by the reason that it is superior to self-lubricating, shock resistance and wear resistance and/or abrasion resistance. In this way, it is expected to propose improving agents which can approve property of each substance in order to make arise a quality of macromolecules substances. Moreover, each polymer in macromolecules substances has a characteristic property itself. For example, ethylene/vinyl acetate copolymer is superior in springiness, elasticity, transparence, stout and heat seal. Polymer in methacrylic acid ester group among methacrylate resins and resins in acrylonitrile group is named generically with metacrylate resin and, they have widely utilized in materials for illumination, commercial advertising panel, car and train, electrical and/or optic materials, daily goods and so on by use of their superior properties such as surface luster, transparence and weather resistance. In addition, other physical properties of polymers is filmed-formation property, rubber-like property, mechanical stout, anti-creep, flexibility, thermoplasticity, thermal resistance, dimensional stability, phase transition, shock resistance, fluidability, surface luster, water resisting property and chemical resistance. Moreover, there are processability, printing, painting, deposition, secondary processing such as lamination, epibole, waterproof, separating, bubble-breaking, oxidation prevention, increasing viscosity, pyrogenetically consolidating property, gelatinization at ordinary temperature, thermal displacement, thermal resistance, alkali resistance, flexural strength, bending elasticity, tug strength, electric characteristics, adhesion, erosion- or rust-resistance, sliding property with thermal resistance, radiation resistance, poly-valenced metal ion capture ability (chelate ability), dispersibility, aggregation ability as another physical properties. Concerning our present social civilization life, these macromolecules substances are necessary and indispensable in our daily life. Thus, it is expected to provide more effective materials which are improved each physical property by combining with each physical property. Polyethylene glycol is one example of the macromolecules which is daily used in general. Application of polyethylene glycol is widely expanded into the manufacturing fields such as cream lotion in cosmetic industry, lubricant in metal processing and/or fiber industry, binder of tablet for pills in pharmaceutic industry and basic material for producing surface-active agents and/or surfactants and, moreover, it is also utilized flocculant for inorganic substances such as clay , resin reform agents (prohydration), thickeners, binders for ceramic, pulp dispersing agents and flocculants for pulp. Then, it is expected to be improved physical property of polyethylene glycol as more safety and effective materials. Moreover, highly polymerized sodium polyethylene acrylic acid is permitted legally as food additive and/or cosmetics material. Thus, it is expected that a proposal of new technique and/or new substance can improve a physical property resulting from change in multi-dimensional structure (conformation) of this polyethylene acryl amide polymer.
In generating property of various types of fibers such as natural fibers in cellulose group, synthetic fibers in hydrocarbon group, synthetic fibers in polyvinyl alcohol group, acrylic synthetic fibers, polyamide synthetic fibers, aramide fibers, synthetic fibers in polyester group, fibers in polyurethane group and carbon fibers, each characteristic feature of those fibers is produced by their molecule configuration and their multi-dimensional structure. Moreover, each physical property of natural gum and synthetic rubber latex, which can produce rubber-like elasticity dependently on given temperature, is also changed by alteration of multi-dimensional structure. Collagen also takes three pairs of right winding spiral structure resulting from formation of left winding helix. Thus, the role of function of this collagen also differs by it""s multi-dimensional structure. Generation of function corresponding to the aim and it""s utilization is also expected by improving the multi-dimensional structure of collagen fibers.
Moreover, there are cosmetic pigments, agents in water-soluble coating materials, scale preventing agents, electroconductive treating agents, stabilizers for emulsion and polymerization, coating materials utilized paint film formation, coating materials of powder, coating materials for radiation consolidation, soluble non-dispersing coating materials and others as another uses of macromolecules. Those are also applied to housing materials, electricity products, motor vehicles, construction materials, furnitures and electric wire insulation mantles and so on. From such reasons, proposal of a new technique and/or a new substance to improve the physical property of these coating materials is prospected.
So, in order to extend utilization of macromolecules, appropriate adhesives is also necessary. To improve function of these adhesives and to efficiently utilize macromolecules substances is expected in various fields such as medical care system, transport system, communication system and constructions.
Moreover, composite materials of macromolecules with specific function is used. The specific function is optical transfer, polarity, recording medium for electronic machines, separating membrane, electrical conductivity, electrical conductivity with transparence, electricity conductivity related to optical radiation, vibration-damping, sound arresting, heat conductivity and so on. Additionally, composite materials of macromolecules with specific function has a possible potential to apply into tip materials such as module for separation, metallizing resins, impact-relaxation materials, vibration-damping conductive materials, optic fibers, magnetic recording medium, optical recording medium, rewritable optical disc. For this reason, a new technique and possible idea which can easily control the function of composite materials as well as change in configuration of the materials are expected in order to make function and performance better.
In addition, functional polymers which can cause a chemical change or a physical change by physical and chemical stimuli externally and which can produce a state change by interaction with a corresponding substance are generated by effects of reactable substrate with specific function which is introduced into main chains and/or side chains of macromolecules or it""s precursor and by a proportional property and specific conformation of an additive. For example, there are materials for electricity, semiconductor related materials, photosensitive polymeric materials, recording materials, materials for liquid crystal display, tip materials, liquid crystal materials of macromolecules, optoelectronics materials, materials for thin films, photochromic materials, optical recording materials, optical tip materials, holographic recording materials, nonlinear optical tip materials, optical responding materials, sensor related materials and transducer related materials as functional polymer composites. Therefore, in order to make well generation, good efficiency and accurate stabilization of each functional property, it is expected to improve function of these polymers. In addition, an improvement of printed circuit board materials for the optical disc which needs property such as transparence, mechanical intensity and thermal resistance and of thin film materials such as the amorphic membrane which polymerized membrane is cross-linked tridimensionality is also expected. Moreover, as an applied example of macromolecules, there is also polymer with photochemistry reaction which causes a configuration change such as cross-linking, polymerization, polarity change, decomposition and depolymerization due to light. Thus, as well as improvement of chemical structure of these photosensitive functional polymers, it is also expected that proposal of a new technique and possible idea which can improve a physical property of materials by changing those conformation.
Moreover, there are also macromolecular substances which have been utilized for detergents, cosmetics and foodstuff. A substance with more useful physical property which results from improving conformation accompanied with generating functional property has been expected to make quality of life and environment better. Additionally, property of macromolecules is utilized as supporting materials in medical health care, then, it is also expected to propose useful and new biomaterials which have better fitness and adaptation to body by improving property of conventional biomaterials which is utilized macromolecules. In addition, there are also stabilizers which makes stability against heat and light, antioxidants (age resistors) which prevents progress of oxidation and ozonolysis, promoting agents which makes plasticity, elasticity and processability well and softener. Moreover, there are also flame retarders with fireresistance, cross-linking agents, fillers, treating agents for fibers, oily agents, electrically charging preventive agents (antistatic agents), final forming agents for flexibility, final forming agents for polymers, additives for plastics, ultraviolet rays absorbents, optical stabilizers, lubricants, curing agents and/or vulcanizing agents, age resistors and softeners. In addition, there are also sclerosing agents and tackifiers, reinforcers, fillers, additives for adhesives, additives for coating materials, cosmetic pigments, solvents, consolidation accelerators, deterioration preventives, dispersing agents as a tool as additives of polymeric materials. Then, it is known well that those are used corresponding to each objective. By improving property of such additives which are used for these polymeric materials, it is expected to provide a new material which has useful functional property.
Moreover, there are various kind of macromolecules for using as detergents, cosmetics and foodstuff. Macromolecules in foodstuff as an example are representative substances such as polysaccharides, foodstuff proteins and macromolecules for gum. Macromolecules for gum, for example, have natural resins such as chicle, soruba and jelutong which contains polyethylene isoprene and which is utilized chewing gum as natural additives. In addition, there are vinyl acetate resin, polyisobutylene, polyethylene butene, isobutyleneisoprene rubber, styrene-butadiene rubber (SBR), polyethylene, terpene resin and so on as food additives. Macromolecules extracted from plants and/or animals as well as synthesized macromolecules are used in detergents and cosmetics. Thus, it is important that in the point of view at better quality of life itself as well as life space, physical property of macromolecular substances is improved it""s conformation generating specific characteristic and function, resulting in being useful one. In addition, an example of utilizing a property of macromolecules as medical care aids materials is a dialysis membrane. As a material of a dialysis membrane, though natural macromolecules (celluloses, cellulose acetate fibers) and synthesized macromolecules (for example, polymethylmethacrylate, polyacrylonitrile, polysulfone, ethylene/vinyl alcohol copolymer) is general purposed, it is also expected to develop a useful and well adapting biomaterials by improving property of these conventional biomaterials. Moreover, prospected additives are antioxidants (or age resistors) which prevent an progress of oxidation and ozonolysis and stabilizers which make stability constant against heat and light. It is also expected to make each performance better by processing a new additive to promoting agents which makes plasticity and/or elasticity, softeners, flame retarders which is added flame-resisting, cross-linking agents (or curing agents and/or vulcanizing agents), fillers, treating agents for fibers, oily agents (for example, spinning oil), antistatic agent (for example, compounds with polyethylene glycol chain, surface-active agents and/or surfactants), final forming agents for flexibility, final forming agents for polymers or additives for plastics. Ultraviolet rays absorbents, optical stabilizers, lubricants, curing agents and/or vulcanizing agents, and age resistors are also important as additives. Softener has an effect as a lubricant in the intermolecular space of gum and has a potency of controlling dispersibility of other additives and, they play a role of increasing in volume of combination agents. In order to produce better physical property such as hardness, tug strength, modulus, anti-elasticity, friction resistance, wear resistance, tear resistance into carbon black and rubber goods, tackifiers and/or reinforcers frequently are added. In addition, fillers, additives for adhesives, additives for coating materials, cosmetic pigments, solvents, sclerosing agents, consolidation accelerators, deterioration preventives, dispersing agents and so on are used as additives of macromolecular materials according to each objective. It is expected to improve property of those additives for various kinds of macromolecular materials as above mentioned.
In conformity with a biological fact mentioned above, it is expected to provide a representative agent and/or drug with the following effects, that can inhibit or block the function generated by multi-dimensional structure of substances which consists of living organism; extracellular matrix, cell membrane, cytoskeleton, cytoplasm and components of intracellular organella such as enzymes, genes, antibody, proteins, sugars, lipids. Those agents and/or drugs are antibacterial agents, antifungal agent, antiviral agent, bactericidal and/or sterilized agents, anticancer drugs, anticoagulants and/or antifibrinolytic agents, blood coagulation and fibrinolysis blocking agents, inhibitory and/or blocking agents of antigen-antibody reaction, organ and/or tissue preservatives, food preservatives. In addition, those agents and/or drugs are also germination or maturation inhibitory agents of fruits and vegetables, antibacterial agents for plastic processing, antimicrobial coating materials, antimicrobial resin waxes, house holding electric instruments, agents for preventing of bacterial and fungal proliferation and/or infection of house furnishings and daily use goods, slime preventing agents for pulp and paper, cleaning agents on field of electronics, agents for preventing bacterial and fungal proliferation and/or infection on metal processing oil (metal working fluid), the agents for preventing bacterial and fungal proliferation and/or infection on the disposal of waste. Moreover, it was hoped for development of inhibitory agents and/or blocking agents of function due to bioactive substances such as enzymes, peptides and genes, spermatocidal agents or contraceptive agents for external use, thrombolytic agents, conformation altering agents of saccharide-chains, agents for preventing arteriosclerosis, metabolism (lipids, sugar, proteins) improving agents, agents for wound healing, epithelialization promoting agents, and inhibitors and/or blocking agents which are able to inhibit or block function generated by the multi-dimensional structure of substance which living organism has many kinds of substrates.
An objective of this invention is to resolve the problems above mentioned, and to provide inhibitory or blocking agents of molecular generating and/or inducing functions, that can inhibit or block functions generated by the multi-dimensional structures of reactive substrates and have a simple chemical structure.
In order to complete the above-mentioned objective, the inventors carried out research and determined that the chemical compounds which are shown in the following general formulae (1-a), (1-b), (2), (3-a) and (3-b) or acid addition salt compounds thereof which are active provide the objective mentioned above.
The invention mentioned in order to complete above-mentioned objective is the inhibitory or blocking agents of molecular generating and/or inducing functions which has the original molecular structure shown in general formula (1-a) (1-b). And, the compounds, the derivatives or those acid addition salt compounds provide antibacterial agents, antifungal agent, antiviral agent, bactericidal and/or sterilized agents, anticancer drugs, blood coagulation and fibrinolysis inhibitors and/or blocking agents, inhibitory and/or blocking agents of antigen-antibody reaction, organ and/or tissue preservatives, antiseptics and preservatives for foodstuffs, germination and maturation inhibitory agents for fruits and vegetables. In addition, the compounds, the derivatives or those acid addition salt compounds provide antibacterial agents for plastic processing, antimicrobial coating materials, antimicrobial resin waxes, agents for preventing of bacterial and fungal proliferation and/or infection of house holding electric instruments, daily use goods and house furnishings, slime preventing agents for papers and pulps, cleaning agents in field of electronics, agents for preventing bacterial and fungal proliferation and/or infection for metal processing oil (metal working fluid), agents for preventing bacterial and fungal proliferation and/or infection for the disposal of waste. In addition, the compounds, the derivatives or those acid addition salt compounds provide spermatocidal agents and/or contraceptive agents which aim to suppress fertility of spermatozoa, thrombolytic agents, conformation altering agents of saccharide-chains, agents for preventing arteriosclerosis, metabolism (lipids, sugar) improving agents, agents for wound healing, epithelialization promoting agents (including hair restoration effect), inhibitors and/or blocking agents which can control generation of function with bioactive substances (for example, enzymes, peptides, gene). In addition, the compounds, the derivatives or those acid addition salt compounds can inhibit and/or block function generated by multi-dimensional structure (conformation) of the substance which consist of a shape and function of living organism. Moreover, the compounds, the derivatives or those acid addition salt compounds provide chemical substances which can control, inhibit and/or block the function which is generated by multi-dimensional structure (conformation) with macromolecules substances and macromolecules composite materials as well as living organism. In addition, when halogen compounds such as halogenated alkali metals or halogenated alkali-earthy metals or halogenated zinc is added in the compounds which were provided by this invention, a reaction is able to be induced. Moreover, when gold colloid is added in the compounds which were provided by this invention, marking and/or labeling substances can be made and, it is also possible to use the compounds which were provided by this invention as dispersion (diffusion) preventives of tinction and printing dye, ink stabilizers or dye sticking agents. In addition, by using a color coupler such as dye with the compounds which were provided by this invention, coloring of the dye can be enhanced. When fragrant agents is used with the compounds which were provided by this invention, possible fragrance can be produced. In addition, the compounds, the derivatives or those acid addition salt compounds can be utilized as depolymerization agents, surface-active agents and/or surfactants, improving agents for surface active substances, phase transition agents, improving agents of phase transition, improving agents of microphase separation structure, plasticity and/or elasticity promoting agents, plasticity and/or elasticity improving agents (plasticizers), copolymerization agents, copolymerization improving agents, improving agents of fluorescent wavelength of colorants, polymerization regulators, improving agents of polymerization adjustment, stabilizers, stabilization improving agents, antioxidants, oxidation preventing agents, agents for improving crystallized materials and/or amorphous materials, fluidability improving agents, flexibility promoters, improving agents for changing flexibility, alterable agents of excitation wavelength, fluorescent wavelength and excitation wavelength of pigmentums, coating materials and cosmetic pigments. And, it is also possible to utilize the compounds, the derivatives or those acid addition salt compounds as the following improving agents. Those are agents which can improve physical property of low molecule substances, agents which can improve function of low molecule substances, agents which can improve physical property of macromolecules substance, agents which can improve function of macromolecules substances, and agents which can improve physical property of macromolecules composite materials and functional macromolecules composite materials. 
However, in the formula,
(i) R1, R2, R3, R4, R5, R6, R10 and R11 represents independently hydrogen atom; halogen atom; C1-C6 alkyl group; amidino group; C3-C8 cycloalkyl group; C1-C6 alkoxy C1-C6 alkyl group; aryl group; allyl group; aralkyl group in which one or more C1-C6 alkyl groups are bound to an aromatic ring selected from the group consisting of benzene, naphthalene and anthracene ring; C1-C6 alkylene group; benzoyl group; cinnamyl group; cinnamoyl group or furoyl group;
(ii) A represents hydrogen atom or 
(wherein
R7 represents C1-C6 alkyl group; sulfide group or phosphate group;
R8 and R9 represent independently hydrogen atom; halogen atom; straight or branched C1-C6 alkyl group; aryl group; allyl group; aralkyl group in which one or more C1-C6 alkyl groups are bound to an aromatic ring selected from the group consisting of benzene, naphthalene and anthracene ring; C1-C6 alkylene group; benzoyl group; cinnamyl group; cinnamoyl group or furoyl group;
(iii) one or more of R1, R2, R3 and R4, and/or one or more of R5, R6, R10 and R11 may be substituted or non-substituted cyclopentyl group; substituted or non-substituted cyclohexyl group; or substituted or non-substituted naphthyl group;
(iv) R5, R6, R10 and R11 may form a ring by binding with another condensation polycyclic hydrocarbon compound or heterocyclic compound;
(v) one or more of R3, R4, R5, R6, R10 and R11 may be substituted by one or more of substituents selected from the group consisting of halogen atom, cyano group, protected or non-protected carboxyl group, protected or non-protected hydroxyl group, protected or non-protected amino group, C1-C6 alkyl group, C1-C6 alkoxy group, C1-C7 alkoxy carbonyl group, aryl group, C3-C6 cycloalkyl group, C1-C6 acylamino group, C1-C6 acyloxy group, C2-C6 alkenyl group, C1-C6 trihalogenoalkyl group, C1-C6 alkylamino group, and C1-C6 dialkylamino group;
(vi) R2 and/or R5 may be substituted by one or more substituents selected from the group consisting of halogen atom, C1-C6 alkyl group, protected or non-protected carboxyl group, protected or non-protected hydroxyl group, protected or non-protected amino group, protected or non-protected C1-C6 alkylamino group, protected or non-protected C1-C6 aminoalkyl group, protected or non-protected C1-C6 alkylamino C1-C6 alkyl group, protected or non-protected hydroxyalkyl group, and C3-C6 cycloalkylamino group;
(vii) when one or more of R3, R4, R5, R6, R10 and R11 are alkyl groups, terminal end(s) of the alkyl group(s) may be substituted by C3-C8 cycloalkyl group).
The aryl group in (i), (ii) and (v) may be phenyl, tollyl, xylyl or naphthyl group. The substituted cyclopentyl group in (iii) may be cyclopentylamino group or cyclopentylcarbinol group, the substituted cyclohexyl group in (iii) may be cyclohexylamino group, cyclohexylaldehyde group or cyclohexyl acetic acid group, and the substituted naphthyl group in (iii) may be naphthylamino group or naphthylamino sulfonic acid group. The condensation polycyclic hydrocarbon compound in (iv) may be pentalene, indene, naphthalene, azulene, heptalene, biphenylene, indacene, acenaphthylene, fluorene, phenalene, phenanthrene, anthracene, pentacene, hexacene, dibenzophenanthrene, 1H-cyclopentacyclooctene or benzocyclooctene, and the heterocyclic compound may be furan, thiophene, pyrrole, xcex3-pyran xcex3-thiopyran, pyridine, thiazole, imidazole pyrimidine, indole or quinoline.
The invention in order to complete above-mentioned objective is the inhibitory or blocking agents of molecular generating and/or inducing function which has the original molecular structure shown in general formula (2). And, the compounds, the derivatives or those acid addition salt compounds with effective integents provide antibacterial agents, antifungal agent, antiviral agent, bactericidal and/or sterilized agents, anticancer drugs, blood coagulation and fibrinolysis inhibitors and/or blocking agents, inhibitory and/or blocking agents of antigen-antibody reaction, organ and/or tissue preservatives, antiseptics and preservatives for foodstuffs, germination and/or maturation inhibitory agents for fruits and vegetables, antibacterial agents for plastic processing, antimicrobial coating materials, antimicrobial resin waxes, agents for preventing of bacterial and fungal proliferation and/or infection of house holding electric instruments, daily use goods and house furnishings, slime preventing agents for papers and pulps, cleaning agents in field of electronics, agents for preventing bacterial and fungal proliferation and/or infection for metal processing oil (metal working fluid), agents for preventing bacterial and fungal proliferation and/or infection for the disposal of waste, spermatocidal agents and/or contraceptive agents which aim to suppress fertility of spermatozoa, thrombolytic agents, conformation altering agents of saccharide-chains, agents for preventing arteriosclerosis, metabolism (lipids, sugar) improving agents, agents for wound healing, epithelialization promoting agents (including hair restoration effect), inhibitors and/or blocking agents which can control generation of function with bioactive substances (for example, enzymes, peptides, genes). In addition, the compounds, the derivatives or those acid addition salt compounds with effective integents can inhibit and/or block function generated by multi-dimensional structure (conformation) of the substance which consist of a shape and function of living organism. Moreover, the compounds, the derivatives or those acid addition salt compounds with effective integents provide chemical substances which can control, inhibit and/or block the function which is generated by multi-dimensional structure (conformation) with macromolecules substances and macromolecules composite materials as well as living organism. In addition, when halogen compounds such as halogenated alkali metals or halogenated alkali-earthy metals or halogenated zinc is added in the compounds which were provided by this invention, a reaction is able to be induced. Moreover, when gold colloid is added in the compounds which were provided by this invention, marking and/or labeling substances can be made and, it is also possible to use the compounds which were provided by this invention as dispersion (diffusion) preventives of tinction and printing dye, ink stabilizers or dye sticking agents. In addition, by using together a color coupler such as dye with the compounds which were provided in this invention, coloring of the dye can be enhanced. When fragrant agents is used with the compounds which were provided by this invention, possible fragrance can be produced. In addition, the compounds, the derivatives or those acid addition salt compounds can be utilized as depolymerization agents, surface-active agents and/or surfactants, improving agents for surface active substances, phase transition agents, improving agents of phase transition, improving agents of microphase separation structure, plasticity and/or elasticity promoting agents, plasticity and/or elasticity improving agents (plasticizers), copolymerization agents, copolymerization improving agents, polymerization regulators, improving agents of polymerization adjustment, stabilizers, stabilization improving agents, antioxidants, oxidation preventing agents, improving agents of crystallized materials and/or amorphous materials, fluidability improving agents, flexibility promoters, improving agents for changing flexibility, improving agents of fluorescent wavelength and excitation wavelength of pigmentums, coating materials, cosmetic pigments and colorants, modulating agents of excitation wavelength and fluorescent wavelength of pigmentums, coating materials, cosmetic pigments and colorants. And, it is also possible to utilize the compounds, the derivatives or those acid addition salt compounds as the following improving agents. Those are agents which can improve physical property of low molecule substances, agents which can improve function of low molecule substances, agents which can improve physical property of macromolecules substance, agents which can improve function of macromolecules substances, agents which can improve physical property of macromolecules composite materials and functional macromolecules composite materials. 
wherein
(i) R1, R2, R3, R4, R5 and R6 represent independently hydrogen atom; halogen atom; C1-C6 alkyl group; amidino group; C3-C8 cycloalkyl group; C1-C6 alkoxy C1-C6 alkyl group; aryl group; allyl group; aralkyl group in which one or more C1-C6 alkyl groups are bound to an aromatic ring selected from the group consisting of benzene, naphthalene and anthracene ring; C1-C6 alkylene group; benzoyl group; cinnamyl group; cinnamoyl group or furoyl group;
(ii) one or more of R1, R2, R3 and R4, and/or one or more of R5 and R6 may be substituted or non-substituted cyclopentyl group; substituted or non-substituted cyclohexyl group; or substituted or non-substituted naphthyl group;
(iii) R5 and R6 may form a ring by binding with another condensation polycyclic hydrocarbon compound or heterocyclic compound;
(iv) one or more of R3, R4, R5 and R6 may be substituted by one or more of substituents selected from the group consisting of halogen atom, cyano group, protected or non-protected carboxyl group, protected or non-protected hydroxyl group, protected or non-protected amino group, C1-C6 alkyl group, C1-C6 alkoxy group, C1-C7 alkoxy carbonyl group, aryl group, C3-C6 cycloalkyl group, C1-C6 acylamino group, C1-C6 acyloxy group, C2-C6 alkenyl group, C1-C6 trihalogenoalkyl group, C1-C6 alkylamino group, and C1-C6 dialkylamino group;
(v) R2 and/or R5 may be substituted by one or more substituents selected from the group consisting of halogen atom, C1-C6 alkyl group, protected or non-protected carboxyl group, protected or non-protected hydroxyl group, protected or non-protected amino group, protected or non-protected C1-C6 alkylamino group, protected or non-protected C1-C6 aminoalkyl group, protected or non-protected C1-C6 alkylamino C1-C6 alkyl group, protected or non-protected hydroxyalkyl group, and C3-C6 cycloalkylamino group;
(vi) when one or more of R3, R4, R5 and R6 are alkyl groups, terminal end(s) of the alkyl group(s) may be substituted by C3-C8 cycloalkyl group).
The aryl group in (i) and (iv) may be phenyl, tollyl, xylyl or naphthyl group. The substituted cyclopentyl group in (ii) may be cyclopentylamino group or cyclopentylcarbinol group, the substituted cyclohexyl group in (ii) may be cyclohexylamino group, cyclohexylaldehyde group or cyclohexyl acetic acid group, and the substituted naphthyl group in (ii) may be naphthylamino group or naphthylamino sulfonic acid group. The condensation polycyclic hydrocarbon compound in (iii) may be pentalene, indene, naphthalene, azulene, heptalene, biphenylene, indacene, acenaphthylene, fluorene, phenalene, phenanthrene, anthracene, pentacene, hexacene, dibenzophenanthrene, 1H-cyclopentacyclooctene or benzocyclooctene, and the heterocyclic compound may be furan, thiophene, pyrrole, xcex3-pyran, xcex3-thiopyran, pyridine, thiazole, imidazole pyrimidine, indole or quinoline.
The invention in order to complete above-mentioned objective is the inhibitory or blocking agents of molecular generating and/or inducing functions which has the original molecular structure shown in general formula (3-a) (3-b). And, the compounds, the derivatives or those acid addition salt compounds with effective integents provide antibacterial agents, antifungal agent, antiviral agent, bactericidal and/or sterilized agents, anticancer drugs, blood coagulation and fibrinolysis inhibitors and/or blocking agents, inhibitory and/or blocking agents of antigen-antibody reaction, organ and/or tissue preservatives, antiseptics and preservatives for foodstuffs, germination and/or maturation inhibitory agents for fruits and vegetables, antibacterial agents for plastic processing, antimicrobial coating materials, antimicrobial resin waxes, agents for preventing of bacterial and fungal proliferation and/or infection of house holding electric instruments, daily use goods and house furnishings, slime preventing agents for papers and pulps, cleaning agents in field of electronics, agents for preventing bacterial and fungal proliferation and/or infection for metal processing oil (metal working fluid), agents for preventing bacterial and fungal proliferation and/or infection for the disposal of waste, spermatocidal agents and/or contraceptive agents which aim to suppress fertility of spermatozoa, thrombolytic agents, conformation altering agents of saccharide-chains, agents for preventing arteriosclerosis, metabolism (lipids, sugar) improving agents, agents for wound healing, epithelialization promoting agents (including hair restoration effect), inhibitors and/or blocking agents which can control generation of function with bioactive substances (for example, enzymes, peptides, gene). In addition, the compounds, the derivatives or those acid addition salt compounds can inhibit and/or block function generated by multi-dimensional structure (conformation) of the substance which consist of a shape and function of living organism. Moreover, the compounds, the derivatives or those acid addition salt compounds provide chemical substances which can control, inhibit and/or block the function which is generated by multi-dimensional structure (conformation) with macromolecules substances and macromolecules composite materials as well as living organism. In addition, when halogen compounds such as halogenated alkali metals or halogenated alkali-earthy metals or halogenated zinc is added in the compounds which were provided by this invention, a reaction is able to be induced. Moreover, when gold colloid is added in the compounds which were provided by this invention, marking and/or labeling substances can be made and, it is also possible to use the compounds which were provided by this invention as dispersion (diffusion) preventives of tinction and printing dye, ink stabilizers or dye sticking agents. In addition, by using a color coupler such as dye with the compounds which were provided by this invention, coloring of the dye can be enhanced. When fragrant agents is used with the compounds which were provided in this invention, possible fragrance can be produced. In addition, the compounds, the derivatives or those acid addition salt compounds can be utilized as depolymerization agents, surface-active agents and/or surfactants, improving agents for surface active substances, phase transition agents, improving agents of phase transition, improving agents of microphase separation structure, plasticity and/or elasticity promoting agents, plasticity and/or elasticity improving agents (plasticizers), copolymerization agents, copolymerization improving agents, polymerization regulators, improving agents of polymerization adjustment, stabilizers, stabilization improving agents, antioxidants, oxidation preventing agents, improving agents of rystallized materials and/or amorphous materials, fluidability improving agents, flexibility promoters, improving agents for changing flexibility, improving agents of fluorescent wavelength and excitation wavelength of pigmentums, coating materials, cosmetic pigments and colorants, alterable agents of fluorescent wavelength and excitation wavelength of pigmentums, coating materials, cosmetic pigments and colorants. And, it is also possible to utilize the compounds, the derivatives or those acid addition salt compounds as the following improving agents. Those are agents which can improve physical property of low molecule substances, agents which can improve function of low molecule substances, agents which can improve physical property of macromolecules substance, agents which can improve function of macromolecules substances, agents which can improve physical property of macromolecules composite materials and functional macromolecules composite materials. 
wherein
(i) R3, R4, R5 and R6 represent independently hydrogen atom; halogen atom; C1-C6 alkyl group; amidino group; C3-C8 cycloalkyl group; C1-C6 alkoxy C1-C6 alkyl group; aryl group; allyl group; aralkyl group in which one or more C1-C6 alkyl groups are bound to an aromatic ring selected from the group consisting of benzene, naphthalene and anthracene ring; C1-C6 alkylene group; benzoyl group; cinnamyl group; cinnamoyl group or furoyl group;
(ii) one or more of R3 and R4, and/or one or more of R5 and R6 may be substituted or non-substituted cyclopentyl group; substituted or non-substituted cyclohexyl group; or substituted or non-substituted naphthyl group;
(iii) R5 and R6 may form a ring by binding with another condensation polycyclic hydrocarbon compound or heterocyclic compound;
(iv) one or more of R3, R4, R5 and R6 may be substituted by one or more of substituents selected from the group consisting of halogen atom, cyano group, protected or non-protected carboxyl group, protected or non-protected hydroxyl group, protected or non-protected amino group, C1-C6 alkyl group, C1-C6 alkoxy group, C1-C7 alkoxy carbonyl group, aryl group, C3-C6 cycloalkyl group, C1-C6 acylamino group, C1-C6 acyloxy group, C2-C6 alkenyl group, C1-C6 trihalogenoalkyl group, C1-C6 alkylamino group, and C1-C6 dialkylamino group;
(v) R5 may be substituted by one or more substituents selected from the group consisting of halogen atom, C1-C6 alkyl group, protected or non-protected carboxyl group, protected or non-protected hydroxyl group, protected or non-protected amino group, protected or non-protected C1-C6 alkylamino group, protected or non-protected C1-C6 aminoalkyl group, protected or non-protected C1-C6 alkylamino C1-C6 alkyl group, protected or non-protected hydroxyalkyl group, and C3-C6 cycloalkylamino group;
(vi) when one or more of R3, R4, R5 and R6 are alkyl groups, terminal end(s) of the alkyl group(s) may be substituted by C3-C8 cycloalkyl group).
The aryl group in (i) and (iv) may be phenyl, tollyl, xylyl or naphthyl group. The substituted cyclopentyl group in (ii) may be cyclopentylamino group or cyclopentylcarbinol group, the substituted cyclohexyl group in (ii) may be cyclohexylamino group, cyclohexylaldehyde group or cyclohexyl acetic acid group, and the substituted naphthyl group in (ii) may be naphthylamino group or naphthylamino sulfonic acid group. The condensation polycyclic hydrocarbon compound in (iii) may be pentalene, indene, naphthalene, azulene, heptalene, biphenylene, indacene, acenaphthylene, fluorene, phenalene, phenanthrene, anthracene, pentacene, hexacene, dibenzophenanthrene, 1H-cyclopentacyclooctene or benzocyclooctene, and the heterocyclic compound may be furan, thiophene, pyrrole, xcex3-pyran, xcex3-thiopyran, pyridine, thiazole, imidazole pyrimidine, indole or quinoline.
The invention provides antibacterial agents, antifungal agents, antiviral agents, bactericidal and/or sterilized agents, anticancer drugs, anticoagulants and/or antifibrinolytic agents, blood coagulation and/or fibrinolysis blocking agents, inhibitory agents of antigen-antibody reaction, preservatives for tissues and/or organs, and antiseptics and preservatives by utilizing effects on change in conformation, thermodynamic effect, phase transition effect, flexibility changing effect, depolymerization effect, improving effect of macromolecules property, chemical kinetic effect, reduction effect, effect as free radical scavengers, desulfurization effect, antioxidant effect, nucleophilic and electrophilic effects according to orbital dynamics of molecules and/or hydrophobic effect, which are inhibitory or blocking agents of molecular generating and/or inducing functions.
The invention provides labeled regents which can detect a targeted position of generating function of molecule, utilizing effect on specific regions due to inhibitory or blocking agents of molecular generating and/or inducing functions, and having a labeled substance at least in one substituent.
The invention provides reductants, free radical scavengers and desufude agents utilizing inhibitory or blocking agents of molecular generating and/or inducing functions.
The invention provides depolymerization agents, improving agents for surface active substances, spermatocidal agents and/or contraceptive agents for external use, thrombolytic agents, conformation altering agents of saccharide-chains, agents for preventing arteriosclerosis, metabolism (lipids, sugar) improving agents, agents for wound healing, epithelialization promoting agents, phase transition agents, improving agents of phase transition, improving agents of microphase separation structure, plasticity and/or elasticity promoting agents, plasticity and/or elasticity improving agents (plasticizers), copolymerization agents, copolymerization improving agents, polymerization regulators, improving agents of polymerization adjustment, stabilizers, stabilization improving agents, antioxidants, oxidation preventing agents, improving agents of crystallized materials and/or amorphous materials, fluidability improving agents, flexibility promoters (softers), improving agents for changing flexibility (softner improving agents), improving agents of excitation wavelength and fluorescent wavelength of colorants, pigmentums, coating materials and cosmetic pigments, and alterable agents of excitation wavelength and fluorescent wavelength of pigmentums, coating materials and cosmetic pigments, agents which can improve physical property of low molecule substances, agents which can improve function of low molecule substances, agents which can improve physical property of macromolecules substance, agents which can improve function of macromolecules substances, agents which can improve physical property of macromolecules composite materials and functional macromolecules composite materials.
In the present specification, unless otherwise specified, the term xe2x80x9chalogen atomxe2x80x9d means, for example, fluorine atom, chlorine atom, bromine atom or iodine atom; the term xe2x80x9calkyl groupxe2x80x9d means C1-10 alkyl group such as methyl group, ethyl group, n-propyl group, isopropyl group, n-butyl group, isobutyl group, sec-butyl group, tort-butyl group, benzyl group, hexyl group, octyl group or the like; the term xe2x80x9clower alkyl groupxe2x80x9d means C1-5 alkyl group among the alkyl groups mentioned above; the term xe2x80x9calkoxy groupxe2x80x9d means xe2x80x94Oxe2x80x94 alkyl group (alkyl group is C1-10 alkyl group mentioned above); the term xe2x80x9clower alkylamino groupxe2x80x9d means C1-5 alkylamino group such as methylamino group, ethylamino group, propylamino group or the like; the term xe2x80x9cdi-lower alkylamino groupxe2x80x9d means C1-5 dialkylamino group such as dimethylamino group; the term xe2x80x9clower alkenyl groupxe2x80x9d means C2-5 alkenyl group such as vinyl group, allyl group, 1-propenyl group, 1-butenyl group or the like; the term xe2x80x9ccycloalkyl groupxe2x80x9d means C3-6 cycloalkyl group such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl or the like; the term xe2x80x9caryl groupxe2x80x9d means, for example, phenyl group or naphthyl group; the term xe2x80x9calkoxy carbonyl groupxe2x80x9d means
xe2x80x94COO-alkyl group (alkyl group means C1-10 alkyl group above mentioned); the term xe2x80x9chydroxy lower alkyl groupxe2x80x9d means hydroxy-C1-5 alkyl group such as hydroxy methyl group, hydroxy ethyl group, hydroxy propyl group or the like; the term xe2x80x9camino lower alkyl groupxe2x80x9d means amino C1-5 alkyl group such as aminomethyl group, aminoethyl group, aminopropyl group or the like; the term xe2x80x9clower alkylamino lower alkyl groupxe2x80x9d means C1-5 alkylamino C1-5 alkyl group such as methylaminomethyl group, ethylaminomethyl group, ethylaminoethyl group or the like; the term xe2x80x9cdi-lower alkylamino lower alkyl groupxe2x80x9d means C1-5 dialkylamino C1-5 alkyl group such as dimethylaminomethyl group or diethylaminomethyl group; the term xe2x80x9ccyclic amino groupxe2x80x9d means cyclic amino group with 4-10 membered ring such as piperazinyl group, morpholinyl group, 1,4-diazabicyclo (3,2,1) octyl group or the like; the term xe2x80x9ccyclic amino lower alkyl groupxe2x80x9d means C1-5 alkyl group attached to cyclic amino group with 4-6 membered ring such as 1-piperazinylmethyl group, 1-pyrrolidinylmethyl group, 1-azethydinylmethyl group, 1-morpholinylmethyl group or the like; the term xe2x80x9cacylamino groupxe2x80x9d means C1-4 acylamino group such as formylamino group, acetylamino group, propionylamino group, butyrylamino group or the like; the term xe2x80x9cacyloxy groupxe2x80x9d means C1-4 acyloxy group such as formyloxy group, acetyloxy group, propionyloxy group, butyryloxy group or the like; the term xe2x80x9ctrihalogeno-lower alkyl groupxe2x80x9d means trihalogeno C1-5 alkyl group such as trichloromethyl group, trifluoromethyl group or the like; the term xe2x80x9cheterocyclic groupxe2x80x9d means 5 membered ring, 6 membered ring or those condensation rings (such as furyl, propyl, thienyl, oxazolyl, imidazolyl, thiazolyl, 1-pyrrolinyl, benzofuryl, benzothiazolyl, pyridyl, quinolyl, pyrimidinyl or morpholinyl group as an example) which has one or more atoms selected from the group consisting of oxygen atom, nitrogen atom and sulfate atom.
The alkyl group represented by R3, R4, R5, R6, R10 or R11 in each general formula may be either straight or branched alkyl group such as, for example, methyl group, ethyl group, propyl group, isopropyl group, butyl isobutyl group, sec-butyl group, 1-butyl group, pentyl group, isopentyl group, neopentyl group or hexyl group which are lower alkyl groups (C1-4). In addition, terminal end of these alkyl groups can be bound to lower cycloalkyl group (C3-4) such as cyclopropyl methyl group, cyclobutyl ethyl group, cyclopentyl methyl group or the like.
Lower cycloalkyl groups (C3-4) included in the cycloalkyl group represented by R3, R4, R5, R6, R10 and R11 in each general formula may be, for example, cyclopropyl group, cyclobutyl group, cyclopentyl group or cyclohexyl group. The alkoxyalkyl group may be, for example, ethyl group, methyl group, methoxyethyl group, ethoxyethyl group, propoxyethyl group, isopropoxyethyl group, butoxyethyl group, methoxypropyl group, 2-ethoxy-1-methyl ethyl group or the like.
Straight or branched alkylene group represented by R3, R4, R5, R6, R10 or R11 in each general formula may be, for example, methylene group, ethylene group, trimethylene group, tetramethylene group, 1,2-dimethylethylene group or the like.
Each substituent of R3, R4, R5, R6, R10 and R11 in each general formula or the methylene group in the general formula 3-a may be at least one substituent selected from the group consisting of halogen atom, cyano group, protected or non-protected carboxyl group, protected or non-protected hydroxyl group, protected or non-protected amino group, alkyl group, alkoxy group, alkoxy carbonyl group, aryl group, cycloalkyl group, acylamino group, acyloxy group, lower alkenyl group, trihalogeno-lower alkyl group, lower alkylamino group, di-lower alkylamino group and the like; R2 and/or R5 may be substituted by at least one substituent selected from the group consisting of halogen atom, lower alkyl group, protected or non-protected carboxyl group, protected or non-protected hydroxyl group, protected or non-protected amino group, protected or non-protected lower alkylamino group, protected or non-protected amino lower alkyl group, protected or non-protected lower alkylamino lower alkyl group, protected or non-protected hydroxy lower alkyl group, di-lower alkylamino group, di-lower alkylamino lower alkyl group or cyclic amino lower alkyl group.
Examples of the protecting substituents of carboxyl group include pharmaceutically acceptable protecting groups of carboxyl group, such as an ester-forming group which is easily detached in an organism.
Moreover, protecting substituent of amino group, amino lower alkyl group, lower alkylamino group, and lower alkylamino lower alkyl group may be a pharmaceutically acceptable amino-protecting group which is easily detached in an organism.
In addition, protecting substituent of hydroxyl group and hydroxy lower alkyl group may be a pharmaceutically acceptable protecting group of hydroxyl group which is easily detached in an organism.
Though halogen compounds can be added to the compositions according to this invention, it is necessary to give heed to an existence of toxicity which the combined compounds may have. By adding halogen compounds, coloring due to light can be prevented. Halogen compounds which can be applied to the compositions according to this invention, for example, are halogenated alkali metals such as potassium bromide, sodium bromide, potassium chloride, sodium chloride, potassium iodide and sodium iodide, and halogenated alkaline-earth metal such as calcium bromide, magnesium bromide, calcium chloride and magnesium chloride, and halogenated zinc such as zinc bromide and zinc chloride.
In addition, in the present specification, unless otherwise specified, or except for the case which is clear from a context, the term xe2x80x9calkyl groupxe2x80x9d includes straight alkyl group as well as branched one. Similarly, the alkyl group in xe2x80x9calkoxy groupxe2x80x9d, xe2x80x9caralkyl groupxe2x80x9d and xe2x80x9calkylamino groupxe2x80x9d which has alkyl group includes straight alkyl group as well as branched one. xe2x80x9cCycloalkyl groupxe2x80x9d is also similar to the above, and includes branched groups such as ethyl cyclopentyl group and methyl cyclohexyl group.
The compounds provided in this invention can be directly applied on the surface of infected wound such as burn and decubitus. And, those can be used by combining with the carrier substances which are allowable on pharmaceutic use. In addition, when it is applied to living space, environment and at industry, those can be used during and/or after manufacturing step of materials according to the objective. Though it is not restricted to representative applications, it is also possible to be added those compounds on any manufacturing steps of surface processing by attaching, painting or spraying as agents to prevent bacterial and fungal proliferation and/or infection for construction materials, furnitures, lavatory goods, bathtub supplies, washing supplies, house holding electric instruments and/or daily use goods. Moreover, when those compounds are utilized in a thread kneading and/or later processing concerning any step of manufacturing fibers and these materials, effect of preventing bacterial and fungal proliferation and/or infection and an anti-allergic effect can be gained. An effect of the objective which is shown by claims can be made by using seats and film materials.
The carrier substances which is allowable on pharmaceutic use are given the carrier substances which is allowable biologically, such as polyoxyalkylenealkyl ether, polyoxyethylene sorbitan fatty acid ester, polyvinylpyrrolidone, hydrocarbon, paraffin, alcohol, polyvalent alcohol, alcohol ester, polyalcohol ester, fatty acid and metal salts of fatty acid. Moreover, chitosan, polyethylene glycol, polyethylene glycerin fatty acid ester (caprylic acid, capric acid, lauric acid) can be exemplified.
In addition, when the compounds mentioned in this invention are used as combined substances with the carrier substances which are allowable on pharmaceutic use, these can be applied in many kinds of the generally known agent types such as cream agents, ointments, pastes, poultices, milky lotions, suspensions, liniments, lotions, aerosol agents, solutions and tapes corresponding to prospected treatments. Also, it is allowed to add solvent supporting agents, isotonic changing agents, pH adjusters, deodorants, antiseptics or odorants in the compounds mentioned in this invention. It is also possible to be added those compounds on any manufacturing steps of surface processing by attaching, painting or spraying as agents to prevent bacterial and fungal proliferation and/or infection for construction materials, furnitures, lavatory goods, bathtub supplies, washing supplies, house holding electric instruments and/or daily use goods. Moreover, when those compounds are utilized in the thread kneading and/or later processing concerning any step of manufacturing fibers and these materials, effect of preventing bacterial and fungal proliferation and/or infection and an anti-allergic effect can be gained. An effect of the objective can be made as wall papers and filters by using seat and film material. When it is used as spermatocidal agents and contraceptive agents for external use, it is also possible to process surface of contraceptive possession such as condoms as well as ointments and creams.
Below, details of this invention are explained. Inhibitory or blocking agents of functions generated by multi-dimensional structure which are used by this invention can be completed above-mentioned objectives by use of the compounds alone, and can be utilized together with acid addition salts, emulsifiers, ester agents or polymerization agents, unless electric charge distribution and electric charge density of molecule are changed drastically. It can be used in the following form as an example; acid addition salts of the compounds which are provided in chemical formula (1-a), (1-b), (2), (3-a) and (3-b) mentioned above are non-toxic salts which are allowable pharmaceutically and, those are inorganic acids such as hydrochloric acid, hydrobromic acid, phosphoric acid or sulfuric acid and organic acids such as acetic acid, citric acid, tartaric acid, lactic acid, succinic acid, fumaric acid, maleic acid or methasulfonic acid.
Concerning chemical formula (1-a) of this invention, the following compounds in chemical formula (1-a) can be given as representatives. But, it is not restricted this invention by the definitive representatives. Concretely, as alkanes which all of R1, R2, R3, R4, R5, R6, R8 and R9 are hydrogen atom and R7 is non-cyclic hydrocarbon, for example, the following compounds are represented.
(1) 4-isopropyl-2-cyclohexen-1-one
(2) 4-isobutyl-2-cyclohexen-1-one
(3) 4-isopentyl-2-cyclohexen-1-one
(4) 4-isohexyl-2-cyclohexen-1-one and so on.
Moreover, as amine-hydrazines which all of R1, R2, R3, R4, R5, R6, R8 and R9 are hydrogen atom and R7 is nitrogen atom, for example,
(5) 4-dimethylamino-2-cyclohexen-1-one
(6) 4-dimethylhydrazono-2-cyclohexen-1-one
(7) 4-isopropylidenehydrazino-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
As phosphines and those analogs which all of R1, R2, R3, R4, R5, R6, R8 and R9 are hydrogen atom and R7 is phosphorus, arsenic or antimony, for example,
(8) 4-dimethylphosphinetolyl-2-cyclohexen-1-one
(9) 4-dimethylallylidenetolyl-2-cyclohexen-1-one
(10) 4-dimethylstibinetolyl-2-cyclohexen-1-one
(11) 4-dimethylbismuthinetriyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
As sulfide compounds which all of R1, R2, R3, R4, R5, R6, R8 and R9 are hydrogen atom and R7 is sulfate, for example,
(12) 4-isopropanesulfo-2-cyclohexen-1-one
(13) 4-isopropanesulfino-2-cyclohexen-1-one
(14) 4-isopropanesulfeno-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
Concerning chemical formula (1-b) of this invention, the following compounds in chemical formula (1-b) can be given as representatives. But, it is not restricted this invention by the definitive representatives. Concretely, as alkanes which all of R1, R2, R3, R4, R5, R6, R8, R9, R10 and R11 are hydrogen atom and R7 is non-cyclic hydrocarbon, for example, the following compounds are represented.
(1) 4-isopropyl-cyclohexane-1-one
(2) 4-isobutyl-cyclohexane-1-one
(3) 4-isopentyl-cyclohexane-1-one
(4) 4-isohexyl-cyclohexane-1-one and so on.
As amine-hydrazines which all of R1, R2, R3, R4, R5, R6, R8, R9, R10 and R11 are hydrogen atom and R7 is nitrogen atom, for example, the following compounds are represented.
(5) 4-dimethylamino-cyclohexane-1-one
(6) 4-dimethylhydrazono-cyclohexane-1-one
(7) 4-isopropylidenehydrazino-cyclohexane-1-one and so on.
As phosphines and analogs which all of R1, R2, R3, R4, R5, R6, R8, R9, R10 and R11 are hydrogen atom and R7 is phosphorus, arsenic or antimony, for example, the following compounds are represented.
(8) 4-dimethylphosphinetriyl-cyclohexane-1-one
(9) 4-dimethylarsinetriyl-cyclohexane-1-one
(10) 4-dimethylstibinetriyl-cyclohexane-1-one
(11) 4-dimethylbismuthinetriyl-cyclohexane-1-one and so on.
As sulfide compounds which all of R1, R2, R3, R4, R5, R6, R8, R9, R10 and R11 are hydrogen atom and R7 is sulfate, for example,
(12) 4-isopropanesulfo-cyclohexane-1-one
(13) 4-isopropanesulfino-cyclohexane-1-one
(14) 4-isopropanesulfeno-cyclohexane-1-one and so on, and those acid addition salts are exemplified.
Concerning chemical formula (2) of this invention, the following compounds in chemical formula (2) can be given as representatives. But, it is not restricted this invention by the definitive representatives. Concretely, as alkanes which all of R3, R4, R5 and R6 are hydrogen atom and R1 and/or R2 are alkyl groups of non-cyclic saturated hydrocarbon, for example,
(15) 4,4,6-trimethyl-2-cyclohexen-1-one
(16) 4,4-dimethyl-6-ethyl-2-cyclohexen-1-one
(17) 4,4-dimethyl-6-propyl-2-cyclohexen-1-one
(18) 4,4-dimethyl-6-isopropyl-2-cyclohexen-1-one
(19) 6-butyl-4,4-dimethyl-2-cyclohexen-1-one
(20) 4,4-dimethyl-6-isobutyl-2-cyclohexen-1-one
(21) 6-benzyl-4,4-dimethyl-2-cyclohexen-1-one
(22) 4,4-dimethyl-6-hexyl-2-cyclohexen-1-one
(23) 4,4-dimethyl-6-octyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
Moreover, when all of R3, R4, R5 and R6 are hydrogen atoms and R1 and/or R2 are alkoxy groups of heterocyclic compounds, for example,
(24) 6-pentyloxy-4,4-dimethyl-2-cyclohexen-1-one
(25) 4,4-dimethyl-6-hexyloxy-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
When all of R3, R4, R5, R6 are hydrogen atoms and R1 and/or R2 are lower alkylamino group of amines, for example,
(26) 4,4-dimethyl-6-methylamino-2-cyclohexen-1-one
(27) 4,4-dimethyl-6-ethylamino-2-cyclohexen-1-one
(28) 4,4-dimethyl-6-propylamino-2-cyclohexen-1-one
(29) 4,4-dimethyl-6-dimethylamino-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
Moreover, when all of R3, R4, R5 and R6 are hydrogen atoms and R1 and/or R2 are alkenyl groups of non-cyclic unsaturation hydrocarbon, for example,
(30) 6-vinyl-4,4-dimethyl-2-cyclohexen-1-one
(31) 6-allyl-4,4-dimethyl-2-cyclohexen-1-one
(32) 4,4-dimethyl-6-isopropenyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
Moreover, when all of R3, R4, R5 and R6 are hydrogen atoms and R1 and/or R2 are cycloalkyl group of monocyclic hydrocarbon, for example,
(32) 6-cyclopropyl-4,4-dimethyl-2-cyclohexen-1-one
(32) 6-cyclobutyl-4,4-dimethyl-2-cyclohexen-1-one
(32) 6-cyclopentyl-4,4-dimethyl-2-cyclohexen-1-one
(32) 6-cyclohexyl-4,4-dimethyl-2-cyclohexen-1-one and so on, and those acid additions are exemplified.
Moreover, when all of R3, R4, R5 and R6 are hydrogen atoms and R1 and/or R2 are allyl group of aromatic hydrocarbon 1 valence group, for example,
(32) 4,4-dimethyl-6-phenyl-2-cyclohexen-1-one
(32) 4,4-dimethyl-6-naphthyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
All of R3, R4, R5 and R6 may be hydrogen atoms and R1 and/or R2 may be alkoxy carbonyl groups as ester. In addition, when all of R3, R4, R5 and R6 are hydrogen atoms and R1 and/or R2 are hydroxy lower alkyl group, for example,
(33) 4,4-dimethyl-6-hydroxymethyl-2-cyclohexen-1-one
(34) 4,4-dimethyl-6-hydroxyethyl-2-cyclohexen-1-one
(35) 4,4-dimethyl-6-hydroxypropyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
Moreover, when all of R3, R4, R5 and R6 are hydrogen atoms and R1 and/or R2 are amino lower alkyl group, for example,
(36) 6-aminomethyl-4,4-dimethyl-2-cyclohexen-1-one
(37) 6-aminoethyl-4,4-dimethyl-2-cyclohexen-1-one
(38) 6-aminopropyl-4,4-dimethyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
Moreover, when all of R3, R4, R5 and R6 are hydrogen atoms and R1 and/or R2 are lower alkylamino lower alkyl group, for example,
(39) 4,4-dimethyl-6-methylaminomethyl-2-cyclohexen-1-one
(40) 4,4-dimethyl-6-ethylaminomethyl-2-cyclohexen-1-one
(41) 4,4-dimethyl-6-ethylaminoethyl-2-cyclohexen-1-one so on, and those acid addition salts are exemplified.
Moreover, when all of R3, R4, R5 and R6 are hydrogen atoms and R1 and/or R2 are di-lower alkylamino lower alkyl group, for example,
(42) 4,4-dimethyl-6-dimethylaminomethyl-2-cyclohexen-1-one
(43) 4,4-dimethyl-6-diethylaminomethyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
Moreover, when all of R3, R4, R5 and R6 are hydrogen atoms and R1 and/or R2 are cyclic amino groups, for example,
(44) 4,4-dimethyl-6-piperazinyl-2-cyclohexen-1-one
(45) 4,4-dimethyl-6-morpholinyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
Moreover, when all of R3, R4, R5 and R6 are hydrogen atoms and R1 and/or R2 are cyclic amino lower alkyl group, for example,
(46) 4,4-dimethyl-6-piperazinylethyl-2-cyclohexen-1-one
(47) 4,4-dimethyl-6-pyrrolinylmethyl-2-cyclohexen-1-one
(48) 6-azethydinylmethyl-4,4-dimethyl-2-cyclohexen-1-one
(49) 4,4-dimethyl-6-morpholinylmethyl-2-cyclohexen-1-one, and so on, and those acid addition salts are exemplified.
Moreover, when all of R3, R4, R5 and R6 are hydrogen atoms and R1 and/or R2 are acylamino group of monoacylamin group, for example,
(50) 4,4-dimethyl-6-formylamino-2-cyclohexen-1-one
(51) 6-acetylamino-4,4-dimethyl-2-cyclohexen-1-one
(52) 4,4-dimethyl-6-propionylamino-2-cyclohexen-1-one
(53) 6-butyrylamino-4,4-dimethyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
Moreover, when all of R3, R4, R5 and R6 are hydrogen atoms and R1 and/or R2 are acyloxy group of ester, for example,
(54) 4,4-dimethyl-6-formyloxy-2-cyclohexen-1-one
(55) 6-acetyloxy-4,4-dimethyl-2-cyclohexen-1-one
(56) 4,4-dimethyl-6-propionyloxy-2-cyclohexen-1-one
(57) 6-butyryloxy-4,4-dimethyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
Moreover, when all of R3, R4, R5 and R6 are hydrogen atoms and R1 and/or R2 are trihalogeno lower alkyl group, for example,
(58) 4,4-dimethyl-6-trichloromethyl-2-cyclohexen-1-one
(59) 4,4-dimethyl-6-trifluoromethyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
Moreover, when all of R3, R4, R5 and R6 are hydrogen atoms and R1 and/or R2 are polycyclic group, for example,
(60) 4,4-dimethyl-6-furyl-2-cyclohexen-1-one
(61) 4,4-dimethyl-6-propyl-2-cyclohexen-1-one
(62) 4,4-dimethyl-6-thienyl-2-cyclohexen-1-one
(63) 4,4-dimethyl-6-isoxazolyl-2-cyclohexen-1-one
(64) 4,4-dimethyl-6-imidazolyl-2-cyclohexen-1-one
(65) 4,4-dimethyl-6-thiazolyl-2-cyclohexen-1-one
(66) 4,4-dimethyl-6-pyrrolinyl-2-cyclohexen-1-one
(67) 6-benzofuryl-4,4-dimethyl-2-cyclohexen-1-one
(68) 6-benzothiazolyl-4,4-dimethyl-2-cyclohexen-1-one
(69) 6-pyridyl-4,4-dimethyl-2-cyclohexen-1-one
(70) 4,4-dimethyl-6-quinolyl-2-cyclohexen-1-one
(71) 4,4-dimethyl-6-pyrimidinyl-2-cyclohexen-1-one
(72) 4,4-dimethyl-6-morpholinyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
Concerning this invention, in the compounds provided by chemical formula (3-a), the compound which all of substituent R3, R4, R5 are R6 in chemical formula (3-a) are hydrogen atoms represents 4,4-dimethyl-6-methylene-2-cyclohexen-1-one, which is termed as Yoshixol. And, as other representatives, the following compounds can be given as representatives. But, it is not restricted this invention by the definitive representatives. Concretely, for example, when all of substituent R3 and/or R4 are alkyl group of non-cyclic saturated hydrocarbon,
(73) 6-methylene-4,4,5-trimethyl-2-cyclohexen-1-one
(74) 4,4-dimethyl-5-ethyl-6-methylene-2-cyclohexen-1-one
(75) 4,4-dimethyl-5-propyl-6-methylene-2-cyclohexen-1-one
(76) 4,4-dimethyl-5-isopropyl-6-methylene-2-cyclohexen-1-one
(77) 5-butyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(78) 4,4-dimethyl-5-isobutyl-6-methylene-2-cyclohexen-1-one
(79) 5-benzyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(80) 4,4-dimethyl-5-hexyl-6-methylene-2-cyclohexen-1-one
(81) 4,4-dimethyl-5-octyl-6-methylene-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R3 and/or R4 are alkoxy group of heterocyclic compound,
(82) 5-pentyloxy-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(83) 4,4-dimethyl-5-hexyloxy-6-methylene-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R3 and/or R4 are lower alkylamino group of amines,
(84) 4,4-dimethyl-5-methylamino-6-methylene-2-cyclohexen-1-one
(85) 4,4-dimethyl-5-ethylamino-6-methylene-2-cyclohexen-1-one
(86) 4,4-dimethyl-5-propylamino-6-methylene-2-cyclohexen-1-one
(87) 4,4-dimethyl-5-dimethylamino-6-methylene-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R3 and/or R4 are alkenyl group of non-cyclic unsaturation hydrocarbon,
(88) 5-vinyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(89) 5-allyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(90) 4,4-dimethyl-5-isopropenyl-6-methylene-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R3 and/or R4 are cycloalkyl group of monocyclic hydrocarbon,
(91) 5-cyclopropyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(92) 5-cyclobutyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(93) 5-cyclopentyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(94) 5-cyclohexyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R3 and/or R4 are allyl group of aromatic hydrocarbon 1 valence group,
(95) 4,4-dimethyl-5-phenyl-6-methylene-2-cyclohexen-1-one
(96) 4,4-dimethyl-5-naphthyl-6-methylene-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
Substituent R3, R4 are sometimes alkoxy carbonyl group aromatic hydrocarbon 1 valence group allyl group of ester.
(98) 4,4-dimethyl-5-hydroxy methyl-6-methylene-2-cyclohexen-1-one
(99) 4,4-dimethyl-5-hydroxy ethyl-6-methylene-2-cyclohexen-1-one
(100) 4,4-dimethyl-5-hydroxy propyl-6-methylene-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R3 and/or R4 are amino lower alkyl group,
(101) 5-aminomethyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(102) 5-aminoethyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(103) 5-aminopropyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R3 and/or R4 are lower alkylamino lower alkyl group,
(104) 4,4-dimethyl-5-methylaminomethyl-6-methylene-2-cyclohexen-1-one
(105) 4,4-dimethyl-5-ethylaminomethyl-6-methylene-2-cyclohexen-1-one
(106) 4,4-dimethyl-5-ethylaminoethyl-6-methylene-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R3 and/or R4 are di-lower alkylamino lower alkyl group,
(107) 4,4-dimethyl-5-dimethylaminomethyl-6-methylene-2-cyclohexen-1-one
(108) 4,4-dimethyl-5-diethylaminomethyl-6-methylene-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R3 and/or R4 are cyclic amino groups,
(109) 4,4-dimethyl-5-piperazinyl-6-methylene-2-cyclohexen-1-one
(110) 4,4-dimethyl-5-morpholinyl-6-methylene-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R3 and/or R4 are cycloamino lower alkyl group,
(111) 4,4-dimethyl-5-piperazinyl ethyl-6-methylene-2-cyclohexen-1-one
(112) 4,4-dimethyl-5-pyrrolinyl methyl-6-methylene-2-cyclohexen-1-one
(113) 5-azethydinylmethyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(114) 4,4-dimethyl-5-morpholinylmethyl-6-methylene-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R3 and/or R4 are acylamino group of monoacylamin group,
(115) 4,4-dimethyl-5-formylamino-6-methylene-2-cyclohexen-1-one
(116) 5-acetylamino-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(117) 4,4-dimethyl-5-propionylamino-6-methylene-2-cyclohexen-1-one
(118) 5-butyrylamino-4,4-dimethyl-6-methylene-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R3 and/or R4 are acyloxy group of ester,
(119) 4,4-dimethyl-5-formyloxy-6-methylene-2-cyclohexen-1-one
(120) 5-acetyloxy-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(121) 4,4-dimethyl-5-propionyloxy-6-methylene-2-cyclohexen-1-one
(122) 5-butyryloxy-4,4-dimethyl-6-methylene-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R3 and/or R4 are trihalogeno lower alkyl group,
(123) 4,4-dimethyl-5-trichloromethyl-6-methylene-2-cyclohexen-1-one
(124) 4,4-dimethyl-5-trifluoromethyl-6-methylene-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R3 and/or R4 are polycyclic group,
(125) 4,4-dimethyl-5-furyl-6-methylene-2-cyclohexen-1-one
(126) 4,4-dimethyl-5-propyl-6-methylene-2-cyclohexen-1-one
(127) 4,4-dimethyl-5-thienyl-6-methylene-2-cyclohexen-1-one
(128) 4,4-dimethyl-5-isoxazolyl-6-methylene-2-cyclohexen-1-one
(129) 4,4-dimethyl-5-imidazolyl-6-methylene-2-cyclohexen-1-one
(130) 4,4-dimethyl-5-thiazolyl-6-methylene-2-cyclohexen-1-one
(131) 4,4-dimethyl-5-pyrrolinyl-6-methylene-2-cyclohexen-1-one
(132) 5-benzofuryl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(133) 5-benzothiazolyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(134) 5-pyridyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(135) 4,4-dimethyl-5-quinolyl-6-methylene-2-cyclohexen-1-one
(136) 4,4-dimethyl-5-pyrimidinyl-6-methylene-2-cyclohexen-1-one
(137) 4,4-dimethyl-5-morpholinyl-6-methylene-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R5 is alkyl group of non-cyclic saturated hydrocarbon,
(138) 3,4,4-trimethyl-6-methylene-2-cyclohexen-1-one
(139) 4,4-dimethyl-3-ethyl-6-methylene-2-cyclohexen-1-one
(140) 4,4-dimethyl-6-methylene-3-propyl-2-cyclohexen-1-one
(141) 4,4-dimethyl-3-isopropyl-6-methylene-2-cyclohexen-1-one
(142) 3-butyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(143) 4,4-dimethyl-3-isobutyl-6-methylene-2-cyclohexen-1-one
(144) 3-benzyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(145) 4,4-dimethyl-3-hexyl-6-methylene-2-cyclohexen-1-one
(146) 4,4-dimethyl-6-methylene-3-octyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R5 is alkoxy group of heterocyclic compound,
(147) 3-pentyloxy-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(148) 4,4-dimethyl-3-hexyloxy-6-methylene -2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R5 is lower alkylamino group of amine group,
(149) 4,4-dimethyl-3-methylamino-6-methylene-2-cyclohexen-1-one
(150) 4,4-dimethyl-3-ethylamino-6-methylene-2-cyclohexen-1-one
(151) 4,4-dimethyl-6-methylene-3-propylamino-2-cyclohexen-1-one
(152) 4,4-dimethyl-3-dimethylamino-6-methylene-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R5 is alkenyl group of non-cyclic unsaturation hydrocarbon,
(153) 3-vinyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(154) 3-allyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(155) 4,4-dimethyl-3-isopropenyl-6-methylene-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R5 is cycloalkyl group of monocyclic hydrocarbon,
(156) 3-cyclopropyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(157) 3-cyclobutyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(158) 3-cyclopentyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(159) 3-cyclohexyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R5 is allyl group of aromatic hydrocarbon 1 valence group,
(160) 4,4-dimethyl-3-phenyl-6-methylene-2-cyclohexen-1-one
(161) 4,4-dimethyl-6-methylene-3-naphthyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
Substituent R5 is alkoxy carbonyl group and the compound becomes ester. For example, when substituent R5 is hydroxy lower alkyl group,
(163) 4,4-dimethyl-3-hydroxy methyl-6-methylene-2-cyclohexen-1-one
(164) 4,4-dimethyl-3-hydroxy ethyl-6-methylene-2-cyclohexen-1-one
(165) 4,4-dimethyl-3-hydroxy propyl-6-methylene-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R5 is an amino lower alkyl group,
(166) 3-aminomethyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(167) 3-aminoethyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(168) 3-aminopropyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R5 is a lower alkylamino lower alkyl group,
(169) 4,4-dimethyl-3-methylaminomethyl-6-methylene-2-cyclohexen-1-one
(170) 4,4-dimethyl-3-ethylaminomethyl-6-methylene-2-cyclohexen-1-one
(171) 4,4-dimethyl-3-ethylaminoethyl-6-methylene-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R5 is a lower alkylamino lower alkyl group,
(172) 3-dimethylaminomethyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(173) 3-diethylaminomethyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R5 is cyclic amino group,
(174) 4,4-dimethyl-6-methylene-3-piperazinyl-2-cyclohexen-1-one
(175) 4,4-dimethyl-6-methylene-3-morpholinyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R5 is cyclic amino lower alkyl group,
(176) 4,4-dimethyl-6-methylene-3-piperazinyl ethyl-2-cyclohexen-1-one
(177) 4,4-dimethyl-6-methylene-3-pyrrolinyl methyl-2-cyclohexen-1-one
(178) 3-azethydinylmethyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(179) 4,4-dimethyl-6-methylene-3-morpholinylmethyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R5 is acylamino group of monoacylamin,
(180) 4,4-dimethyl-3-formylamino-6-methylene-2-cyclohexen-1-one
(181) 3-acetylamino-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(182) 4,4-dimethyl-6-methylene-3-propionylamino-2-cyclohexen-1-one
(183) 3-butyrylamino-4,4-dimethyl-6-methylene-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R5 is acyloxy group of ester,
(184) 4,4-dimethyl-3-formyloxy-6-methylene-2-cyclohexen-1-one
(185) 3-acetyloxy-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(186) 4,4-dimethyl-6-methylene-3-propionyloxy-2-cyclohexen-1-one
(187) 3-butyryloxy-4,4-dimethyl-6-methylene-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R5 is a trihalogeno lower alkyl group,
(188) 4,4-dimethyl-6-methylene-3-trichloromethyl-2-cyclohexen-1-one
(189) 4,4-dimethyl-6-methylene-3-trifluoromethyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R5 is polycyclic group,
(190) 4,4-dimethyl-3-furyl-6-methylene-2-cyclohexen-1-one
(191) 4,4-dimethyl-6-methylene-3-propyl-2-cyclohexen-1-one
(192) 4,4-dimethyl-6-methylene-3-thienyl-2-cyclohexen-1-one
(193) 4,4-dimethyl-3-isoxazolyl-6-methylene-2-cyclohexen-1-one
(194) 4,4-dimethyl-3-imidazolyl-6-methylene-2-cyclohexen-1-one
(195) 4,4-dimethyl-6-methylene-3-thiazolyl-2-cyclohexen-1-one
(196) 4,4-dimethyl-6-methylene-3-pyrrolinyl-2-cyclohexen-1-one
(197) 3-benzofuryl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(198) 3-benzothiazolyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(199) 3-pyridyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(200) 4,4-dimethyl-6-methylene-3-quinolyl-2-cyclohexen-1-one
(201) 4,4-dimethyl-6-methylene-3-pyrimidinyl-2-cyclohexen-1-one
(202) 4,4-dimethyl-6-methylene-3-morpholinyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R6 is alkyl group of non-cyclic saturated hydrocarbon,
(203) 6-methylene-2,4,4-trimethyl-2-cyclohexen-1-one
(204) 4,4-dimethyl-2-ethyl-6-methylene-2-cyclohexen-1-one
(205) 4,4-dimethyl-6-methylene-2-propyl-2-cyclohexen-1-one
(206) 4,4-dimethyl-2-isopropyl-6-methylene-2-cyclohexen-1-one
(207) 2-butyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(208) 4,4-dimethyl-2-isobutyl-6-methylene-2-cyclohexen-1-one
(209) 2-benzyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(210) 4,4-dimethyl-2-hexyl-6-methylene-2-cyclohexen-1-one
(211) 4,4-dimethyl-6-methylene-2-octyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R6 is alkoxy group of heterocyclic compound,
(212) 2-pentyloxy-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(213) 4,4-dimethyl-2-hexyloxy-6-methylene-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R6 is a lower alkylamino group of amines,
(214) 4,4-dimethyl-2-methylamino-6-methylene-2-cyclohexen-1-one
(215) 4,4-dimethyl-2-ethylamino-6-methylene-2-cyclohexen-1-one
(216) 4,4-dimethyl-6-methylene-2-propylamino-2-cyclohexen-1-one
(217) 2-dimethylamino-4,4-dimethyl-6-methylene-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R6 is alkenyl group of non-cyclic saturated hydrocarbon,
(218) 2-vinyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(219) 2-allyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(220) 4,4-dimethyl-2-isopropenyl-6-methylene-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R6 is cycloalkyl group of monocyclic hydrocarbon,
(221) 2-cyclopropyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(222) 2-cyclobutyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(223) 2-cyclopentyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(224) 2-cyclohexyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R6 is allyl group of aromatic hydrocarbon 1 valence group,
(225) 4,4-dimethyl-2-phenyl-6-methylene-2-cyclohexen-1-one
(226) 4,4-dimethyl-6-methylene-2-naphthyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
Substituent R6 is alkoxy carbonyl group resulting in ester. For example, when substituent R6 is a hydroxy lower alkyl group,
(228) 4,4-dimethyl-2-hydroxy methyl-6-methylene-2-cyclohexen-1-one
(229) 4,4-dimethyl-2-hydroxy ethyl-6-methylene-2-cyclohexen-1-one
(230) 4,4-dimethyl-2-hydroxy propyl-6-methylene-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R6 is an amino lower alkyl group,
(231) 2-aminomethyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(232) 2-aminoethyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(233) 2-aminopropyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R6 is a lower alkylamino lower alkyl group,
(234) 4,4-dimethyl-2-methylaminomethyl-6-methylene-2-cyclohexen-1-one
(235) 4,4-dimethyl-2-ethylaminomethyl-6-methylene-2-cyclohexen-1-one
(236) 4,4-dimethyl-2-ethylaminoethyl-6-methylene-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R6 is a di-lower alkylamino lower alkyl group,
(237) 2-dimethylaminomethyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(238) 2-diethylaminomethyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R6 is cyclic amino group,
(239) 4,4-dimethyl-6-methylene-2-piperazinyl-2-cyclohexen-1-one
(240) 4,4-dimethyl-6-methylene-2-morpholinyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R6 is a cyclic amino lower alkyl group,
(241) 4,4-dimethyl-6-methylene-2-piperazinyl ethyl-2-cyclohexen-1-one
(242) 4,4-dimethyl-6-methylene-2-pyrrolinyl methyl-2-cyclohexen-1-one
(243) 2-azethydinylmethyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(244) 4,4-dimethyl-6-methylene-2-morpholinylmethyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R6 is acylamino group of monoacylamin,
(245) 4,4-dimethyl-2-formylamino-6-methylene-2-cyclohexen-1-one
(246) 2-acetylamino-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(247) 4,4-dimethyl-6-methylene-2-propionylamino-2-cyclohexen-1-one
(248) 2-butyrylamino-4,4-dimethyl-6-methylene-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R6 is acyloxy group of ester,
(249) 4,4-dimethyl-2-formyloxy-6-methylene-2-cyclohexen-1-one
(250) 2-acetyloxy-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(251) 4,4-dimethyl-6-methylene-2-propionyloxy-2-cyclohexen-1-one
(252) 2-butyryloxy-4,4-dimethyl-6-methylene-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R6 is a trihalogeno lower alkyl group,
(253) 4,4-dimethyl-6-methylene-2-trichloromethyl-2-cyclohexen-1-one
(254) 4,4-dimethyl-6-methylene-2-trifluoromethyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified. For example, when substituent R6 is polycyclic group,
(255) 4,4-dimethyl-2-furyl-6-methylene-2-cyclohexen-1-one
(256) 4,4-dimethyl-6-methylene-2-propyl-2-cyclohexen-1-one
(257) 4,4-dimethyl-6-methylene-2-thienyl-2-cyclohexen-1-one
(258) 4,4-dimethyl-2-isoxazolyl-6-methylene-2-cyclohexen-1-one
(259) 4,4-dimethyl-2-imidazolyl-6-methylene-2-cyclohexen-1-one
(260) 4,4-dimethyl-6-methylene-2-thiazolyl-2-cyclohexen-1-one
(261) 4,4-dimethyl-6-methylene-2-pyrrolinyl-2-cyclohexen-1-one
(262) 2-benzofuryl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(263) 2-benzothiazolyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(264) 2-pyridyl-4,4-dimethyl-6-methylene-2-cyclohexen-1-one
(265) 4,4-dimethyl-6-methylene-2-quinolyl-2-cyclohexen-1-one
(267) 4,4-dimethyl-6-methylene-2-pyrimidinyl-2-cyclohexen-1-one
(268) 4,4-dimethyl-6-methylene-2-morpholinyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when R5 and/or R6 in chemical formula (3-a) are bond substituent such as condensation polycyclic hydrocarbons and heterocyclic compounds,
(269) 5H-4-dimethyl-6-methylene-7-oxo-indene
(270) 4-dimethyl-2-methylene-1-oxo-tetralin
(271) 3H-4-dimethyl-2-methylene-1-oxo-anthracene
(272) 5H-4-dimethyl-6-methylene-7-oxo-benzothiophene
(273) 5H-4-dimethyl-6-methylene-7-oxo-benzofuran
(274) 5H-4-dimethyl-6-methylene-7-oxo-indole
(275) 6H-5-dimethyl-7-methylene-8-oxo-quinoline
(276) 6H-5-dimethyl-7-methylene-8-oxo-quinoxaline
(277) 6H-5-dimethyl-7-methylene-8-oxo-cinnoline
(278) 5H-5-dimethyl-7-methylene-8-oxo-1,4 dithianaphthalene
(279) 3H-4-dimethyl-2-methylene-1-oxo-thianthrene and so on, and those acid addition salts are exemplified.
Concerning this invention, in the compounds provided by chemical formula (3-b), the compound which all of substituent R3, R4, R5 are R6 in chemical formula (3-b) are hydrogen atoms represents 4,4-dimethyl-2-cyclohexen-1-one. And, as other representatives, the following compounds can be given as representatives. But, it is not restricted this invention by the definitive representatives.
Concretely, when all of substituent R3 and/or R4 are alkyl group of non-cyclic saturated hydrocarbon,
(280) 4,4,5-trimethyl-2-cyclohexen-1-one
(281) 4,4-dimethyl-5-ethyl-2-cyclohexen-1-one
(282) 4,4-dimethyl-5-propyl-2-cyclohexen-1-one
(283) 4,4-dimethyl-5-isopropyl-2-cyclohexen-1-one
(284) 5-butyl-4,4-dimethyl-2-cyclohexen-1-one
(285) 4,4-dimethyl-5-isobutyl-2-cyclohexen-1-one
(286) 5-benzyl-4,4-dimethyl-2-cyclohexen-1-one
(287) 4,4-dimethyl-5-hexyl-2-cyclohexen-1-one
(288) 4,4-dimethyl-5-octyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R3 and/or R4 are alkoxy groups of heterocyclic compound,
(289) 5-pentyloxy-4,4-dimethyl-2-cyclohexen-1-one
(290) 4,4-dimethyl-5-hexyloxy-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified. For example, when substituent R3 and/or R4 are lower alkylamino group of amines,
(291) 4,4-dimethyl-5-methylamino-2-cyclohexen-1-one
(292) 4,4-dimethyl-5-ethylamino-2-cyclohexen-1-one
(293) 4,4-dimethyl-5-propylamino-2-cyclohexen-1-one
(294) 4,4-dimethyl-5-dimethylamino-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R3 and/or R4 are alkenyl group of non-cyclic unsaturation hydrocarbon,
(295) 5-vinyl-4,4-dimethyl-2-cyclohexen-1-one
(296) 5-allyl-4,4-dimethyl-2-cyclohexen-1-one
(297) 4,4-dimethyl-5-isopropenyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R3 and/or R4 are cycloalkyl group of monocyclic hydrocarbon,
(298) 5-cyclopropyl-4,4-dimethyl-2-cyclohexen-1-one
(299) 5-cyclobutyl-4,4-dimethyl-2-cyclohexen-1-one
(300) 5-cyclopentyl-4,4-dimethyl-2-cyclohexen-1-one
(301) 5-cyclohexyl-4,4-dimethyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R3 and/or R4 are allyl group of aromatic hydrocarbon 1 valence group,
(302) 4,4-dimethyl-5-phenyl-2-cyclohexen-1-one
(303) 4,4-dimethyl-5-naphthyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified. Substituent R3 and/or R4 are sometimes alkoxy carbonyl aromatic hydrocarbon 1 valence group and/or allyl group of ester.
(305) 4,4-dimethyl-5-hydroxy methyl-2-cyclohexen-1-one
(306) 4,4-dimethyl-5-hydroxy ethyl-2-cyclohexen-1-one
(307) 4,4-dimethyl-5-hydroxy propyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R3 and/or R4 are amino lower alkyl group,
(308) 5-aminomethyl-4,4-dimethyl-2-cyclohexen-1-one
(309) 5-aminoethyl-4,4-dimethyl-2-cyclohexen-1-one
(310) 5-aminopropyl-4,4-dimethyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R3 and/or R4 are lower alkylamino lower alkyl group,
(311) 4,4-dimethyl-5-methylaminomethyl-2-cyclohexen-1-one
(312) 4,4-dimethyl-5-ethylaminomethyl-2-cyclohexen-1-one
(313) 4,4-dimethyl-5-ethylaminoethyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R3 and/or R4 are di-lower alkylamio lower alkyl group,
(314) 4,4-dimethyl-5-dimethylaminomethyl-2-cyclohexen-1-one
(315) 4,4-dimethyl-5-diethylaminomethyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R3 and/or R4 are cyclic amino groups,
(316) 4,4-dimethyl-5-piperazinyl-2-cyclohexen-1-one
(317) 4,4-dimethyl-5-morpholinyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R3 and/or R4 are cyclic amino lower alkyl group,
(318) 4,4-dimethyl-5-piperazinyl ethyl-2-cyclohexen-1-one
(319) 4,4-dimethyl-5-pyrrolinyl methyl-2-cyclohexen-1-one
(320) 5-azethydinylmethyl-4,4-dimethyl-2-cyclohexen-1-one
(321) 4,4-dimethyl-5-morpholinylmethyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R3 and/or R4 are acylamino groups of monoacylamin,
(322) 4,4-dimethyl-5-formylamino-2-cyclohexen-1-one
(323) 5-acetylamino-4,4-dimethyl-2-cyclohexen-1-one
(324) 4,4-dimethyl-5-propionylamino-2-cyclohexen-1-one
(325) 5-butyrylamino-4,4-dimethyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R3 and/or R4 are acyloxy group of ester,
(326) 4,4-dimethyl-5-formyloxy-2-cyclohexen-1-one
(327) 5-acetyloxy-4,4-dimethyl-2-cyclohexen-1-one
(328) 4,4-dimethyl-5-propionyloxy-2-cyclohexen-1-one
(329) 5-butyryloxy-4,4-dimethyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R3 and/or R4 are trihalogeno lower alkyl group,
(330) 4,4-dimethyl-5-trichloromethyl-2-cyclohexen-1-one
(331) 4,4-dimethyl-5-trifluoromethyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R3 and/or R4 are polycyclic groups,
(332) 4,4-dimethyl-5-furyl-2-cyclohexen-1-one
(333) 4,4-dimethyl-5-propyl-2-cyclohexen-1-one
(334) 4,4-dimethyl-5-thienyl-2-cyclohexen-1-one
(335) 4,4-dimethyl-5-isoxazolyl-2-cyclohexen-1-one
(336) 4,4-dimethyl-5-imidazolyl-2-cyclohexen-1-one
(337) 4,4-dimethyl-5-thiazolyl-2-cyclohexen-1-one
(338) 4,4-dimethyl-5-pyrrolinyl-2-cyclohexen-1-one
(339) 5-benzofuryl-4,4-dimethyl-2-cyclohexen-1-one
(340) 5-benzothiazolyl-4,4-dimethyl-2-cyclohexen-1-one
(341) 5-pyridyl-4,4-dimethyl-2-cyclohexen-1-one
(342) 4,4-dimethyl-5-quinolyl-2-cyclohexen-1-one
(343) 4,4-dimethyl-5-pyrimidinyl-2-cyclohexen-1-one
(344) 4,4-dimethyl-5-morpholinyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R5 is alkyl group of non-cyclic saturated hydrocarbon,
(345) 3,4,4-trimethyl-2-cyclohexen-1-one
(346) 4,4-dimethyl-3-ethyl-2-cyclohexen-1-one
(347) 4,4-dimethyl-3-propyl-2-cyclohexen-1-one
(348) 4,4-dimethyl-3-isopropyl-2-cyclohexen-1-one
(349) 3-butyl-4,4-dimethyl-2-cyclohexen-1-one
(350) 4,4-dimethyl-3-isobutyl-2-cyclohexen-1-one
(351) 3-benzyl-4,4-dimethyl-2-cyclohexen-1-one
(352) 4,4-dimethyl-3-hexyl-2-cyclohexen-1-one
(353) 4,4-dimethyl-3-octyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R5 is alkoxy group of heterocyclic compound,
(354) 3-pentyloxy-4,4-dimethyl-2-cyclohexen-1-one
(355) 4,4-dimethyl-3-hexyloxy-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified. For example, when substituent R5 is a lower alkylamino group of amines,
(356) 4,4-dimethyl-3-methylamino-2-cyclohexen-1-one
(357) 4,4-dimethyl-3-ethylamino-2-cyclohexen-1-one
(358) 4,4-dimethyl-3-propylamino-2-cyclohexen-1-one
(359) 3-dimethylamino-4,4-dimethyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R5 is alkenyl group of non-cyclic unsaturation hydrocarbon,
(360) 3-vinyl-4,4-dimethyl-2-cyclohexen-1-one
(361) 3-allyl-4,4-dimethyl-2-cyclohexen-1-one
(362) 4,4-dimethyl-3-isopropenyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R5 is cycloalkyl group of monocyclic hydrocarbon,
(363) 3-cyclopropyl-4,4-dimethyl-2-cyclohexen-1-one
(364) 3-cyclobutyl-4,4-dimethyl-2-cyclohexen-1-one
(365) 3-cyclopentyl-4,4-dimethyl-2-cyclohexen-1-one
(366) 3-cyclohexyl-4,4-dimethyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R5 is allyl group of aromatic hydrocarbon 1 valence group,
(367) 4,4-dimethyl-3-phenyl-2-cyclohexen-1-one
(368) 4,4-dimethyl-3-naphthyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified. Substituent R5 is alkoxy carbonyl group resulting in ester.
For example, when substituent R5 is hydroxy lower alkyl group,
(370) 4,4-dimethyl -3-hydroxy methyl-2-cyclohexen-1-one
(371) 4,4-dimethyl -3-hydroxy ethyl-2-cyclohexen-1-one
(372) 4,4-dimethyl -3-hydroxy propyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R5 is amino lower alkyl group,
(373) 3-aminomethyl-4,4-dimethyl-2-cyclohexen-1-one
(374) 3-aminoethyl-4,4-dimethyl-2-cyclohexen-1-one
(375) 3-aminopropyl-4,4-dimethyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R5 is a lower alkylamino lower alkyl group,
(376) 4,4-dimethyl-3-methylaminomethyl-2-cyclohexen-1-one
(377) 4,4-dimethyl-3-ethylaminomethyl-2-cyclohexen-1-one
(378) 4,4-dimethyl-3-ethylaminoethyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R5 is a di-lower alkylamino lower alkyl group,
(379) 3-dimethylaminomethyl-4,4-dimethyl-2-cyclohexen-1-one
(380) 3-diethylaminomethyl-4,4-dimethyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R5 is cyclic amino group,
(381) 4,4-dimethyl-3-piperazinyl-2-cyclohexen-1-one
(382) 4,4-dimethyl-3-morpholinyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R5 is a cyclic amino lower alkyl group,
(383) 4,4-dimethyl-3-piperazinylethyl-2-cyclohexen-1-one
(384) 4,4-dimethyl-3-pyrrolinylmethyl-2-cyclohexen-1-one
(385) 3-azethydinylmethyl-4,4-dimethyl-2-cyclohexen-1-one
(386) 4,4-dimethyl-3-morpholinylmethyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R5 is acylamino group of monoacylamin,
(387) 4,4-dimethyl-3-formylamino-2-cyclohexen-1-one
(388) 3-acetylamino-4,4-dimethyl-2-cyclohexen-1-one
(389) 4,4-dimethyl-3-propionylamino-2-cyclohexen-1-one
(390) 3-butyrylamino-4,4-dimethyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R5 is acyloxy group of ester,
(391) 4,4-dimethyl-3-formyloxy-2-cyclohexen-1-one
(392) 3-acetyloxy-4,4-dimethyl-2-cyclohexen-1-one
(393) 4,4-dimethyl-3-propionyloxy-2-cyclohexen-1-one
(394) 3-butyryloxy-4,4-dimethyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R5 is a trihalogeno lower alkyl group,
(395) 4,4-dimethyl-3-trichloromethyl-2-cyclohexen-1-one
(396) 4,4-dimethyl-3-trifluoromethyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R5 is polycyclic group,
(397) 4,4-dimethyl-3-furyl-2-cyclohexen-1-one
(398) 4,4-dimethyl-3-propyl-2-cyclohexen-1-one
(399) 4,4-dimethyl-3-thienyl-2-cyclohexen-1-one
(400) 4,4-dimethyl-3-isoxazolyl-2-cyclohexen-1-one
(401) 4,4-dimethyl-3-imidazolyl-2-cyclohexen-1-one
(402) 4,4-dimethyl-3-thiazolyl-2-cyclohexen-1-one
(403) 4,4-dimethyl-3-pyrrolinyl-2-cyclohexen-1-one
(404) 3-benzofuryl-4,4-dimethyl-2-cyclohexen-1-one
(405) 3-benzothiazolyl-4,4-dimethyl-2-cyclohexen-1-one
(406) 3-pyridyl-4,4-dimethyl-2-cyclohexen-1-one
(407) 4,4-dimethyl-3-quinolyl-2-cyclohexen-1-one
(408) 4,4-dimethyl-3-pyrimidinyl-2-cyclohexen-1-one
(409) 4,4-dimethyl-3-morpholinyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R6 is alkyl group of non-cyclic saturated hydrocarbon,
(410) 2,4,4-trimethyl-2-cyclohexen-1-one
(411) 4,4-dimethyl-2-ethyl-2-cyclohexen-1-one
(412) 4,4-dimethyl-2-propyl-2-cyclohexen-1-one
(413) 4,4-dimethyl-2-isopropyl-2-cyclohexen-1-one
(414) 2-butyl-4,4-dimethyl-2-cyclohexen-1-one
(415) 4,4-dimethyl-2-isobutyl-2-cyclohexen-1-one
(416) 2-benzyl-4,4-dimethyl-2-cyclohexen-1-one
(417) 4,4-dimethyl-2-hexyl-2-cyclohexen-1-one
(418) 4,4-dimethyl-2-octyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R6 is alkoxy group of heterocyclic compound,
(419) 2-pentyloxy-4,4-dimethyl-2-cyclohexen-1-one
(420) 4,4-dimethyl-2-hexyloxy-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified. For example, when substituent R6 is a lower alkylamino group of amines,
(421) 4,4-dimethyl-2-methylamino-2-cyclohexen-1-one
(422) 4,4-dimethyl-2-ethylamino-2-cyclohexen-1-one
(423) 4,4-dimethyl-2-propylamino-2-cyclohexen-1-one
(424) 2-dimethylamino-4,4-dimethyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R6 is alkenyl group of non-cyclic saturated hydrocarbon,
(425) 2-vinyl-4,4-dimethyl-2-cyclohexen-1-one
(426) 2-allyl-4,4-dimethyl-2-cyclohexen-1-one
(427) 4,4-dimethyl-2-isopropenyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R6 is cycloalkyl group of single cyclic hydrocarbon,
(428) 2-cyclopropyl-4,4-dimethyl-2-cyclohexen-1-one
(429) 2-cyclobutyl-4,4-dimethyl-2-cyclohexen-1-one
(430) 2-cyclopentyl-4,4-dimethyl-2-cyclohexen-1-one
(431) 2-cyclohexyl-4,4-dimethyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R6 is allyl group of aromatic hydrocarbon 1 valence group,
(432) 4,4-dimethyl-2-phenyl-2-cyclohexen-1-one
(433) 4,4-dimethyl-2-naphthyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified. Substituent R6 represents alkoxy carbonyl group and sometimes becomes ester.
For example, when substituent R6 is a hydroxy lower alkyl group,
(435) 4,4-dimethyl-2-hydroxy methyl-2-cyclohexen-1-one
(436) 4,4-dimethyl -2-hydroxy ethyl-2-cyclohexen-1-one
(437) 4,4-dimethyl -2-hydroxy propyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R6 is an amino lower alkyl group,
(438) 2-aminomethyl-4,4-dimethyl-2-cyclohexen-1-one
(439) 2-aminoethyl-4,4-dimethyl-2-cyclohexen-1-one
(440) 2-aminopropyl-4,4-dimethyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R6 is a lower alkylamino lower alkyl group,
(441) 4,4-dimethyl-2-methylaminomethyl-2-cyclohexen-1-one
(442) 4,4-dimethyl-2-ethylaminomethyl-2-cyclohexen-1-one
(443) 4,4-dimethyl-2-ethylaminoethyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R6 is a di-lower alkylamino lower alkyl group,
(444) 2-dimethylaminomethyl-4,4-dimethyl-2-cyclohexen-1-one
(445) 2-diethylaminomethyl-4,4-dimethyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R6 is cyclic amino group,
(446) 4,4-dimethyl-2-piperazinyl-2-cyclohexen-1-one
(447) 4,4-dimethyl-2-morpholinyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R6 is a cyclic amino lower alkyl group,
(448) 4,4-dimethyl-2-piperazinylethyl-2-cyclohexen-1-one
(449) 4,4-dimethyl-2-pyrrolinylmethyl-2-cyclohexen-1-one
(450) 2-azethydinylmethyl-4,4-dimethyl-2-cyclohexen-1-one
(451) 4,4-dimethyl-2-morpholinylmethyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R6 is acylamino group of monoacylamin,
(452) 4,4-dimethyl-2-formylamino-2-cyclohexen-1-one
(453) 2-acetylamino-4,4-dimethyl-2-cyclohexen-1-one
(454) 4,4-dimethyl-2-propionylamino-2-cyclohexen-1-one
(455) 2-butyrylamino-4,4-dimethyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R6 is acyloxy group of ester,
(456) 4,4-dimethyl-2-formyloxy-2-cyclohexen-1-one
(457) 2-acetyloxy-4,4-dimethyl-2-cyclohexen-1-one
(458) 4,4-dimethyl-2-propionyloxy-2-cyclohexen-1-one
(459) 2-butyryloxy-4,4-dimethyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R6 is a trihalogeno lower alkyl group,
(460) 4,4-dimethyl-2-trichloromethyl-2-cyclohexen-1-one
(461) 4,4-dimethyl-2-trifluoromethyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when substituent R6 is polycyclic group,
(462) 4,4-dimethyl-2-furyl-2-cyclohexen-1-one
(463) 4,4-dimethyl-2-propyl-2-cyclohexen-1-one
(464) 4,4-dimethyl-2-thienyl-2-cyclohexen-1-one
(465) 4,4-dimethyl-2-isoxazolyl-2-cyclohexen-1-one
(466) 4,4-dimethyl-2-imidazolyl-2-cyclohexen-1-one
(467) 4,4-dimethyl-2-thiazolyl-2-cyclohexen-1-one
(468) 4,4-dimethyl-2-pyrrolinyl-2-cyclohexen-1-one
(469) 2-benzofuryl-4,4-dimethyl-2-cyclohexen-1-one
(470) 2-benzothiazolyl-4,4-dimethyl-2-cyclohexen-1-one
(471) 2-pyridyl-4,4-dimethyl-2-cyclohexen-1-one
(472) 4,4-dimethyl-2-quinolyl-2-cyclohexen-1-one
(473) 4,4-dimethyl-2-pyrimidinyl-2-cyclohexen-1-one
(474) 4,4-dimethyl-2-morpholinyl-2-cyclohexen-1-one and so on, and those acid addition salts are exemplified.
For example, when R5 and/or R6 in chemical formula (3-b) are bond substituents of condensation polycyclic hydrocarbon compounds and condensation heterocyclic compounds,
(475) 5H-4-dimethyl-7-oxo-indene
(476) 4-dimethyl-1-oxo-tetralin
(477) 3H-4-dimethyl-1-oxo-anthracene
(478) 5H-4-dimethyl-7-oxo-benzothiophene
(479) 5H-4-dimethyl-7-oxo-benzofuran
(480) 5H-4-dimethyl-7-oxo-indole
(481) 6H-5-dimethyl-8-oxo-quinoline
(482) 6H-5-dimethyl-8-oxo-quinoxaline
(483) 6H-5-dimethyl-8-oxo-cinnoline
(484) 5H-5-dimethyl-8-oxo-1,4-dithianaphthalene
(485) 3H-4-dimethyl-1-oxo-thianthrene, and those acid addition salts are exemplified.
The compounds which is shown in chemical formula (1-a), (1-b), (2), (3-a) and (3-b) of this invention can be synthesized by the known processing manners of organic synthesis with conventional organic chemical compounds and/or natural plant oils. When the acid addition salts or the compounds which is shown in general formula (1-a), (1-b), (2), (3-a) and (3-b) are used as inhibitory or blocking agents of function which is generated by multi-dimensional structure, it is possible to be administered as a single agent or a combined agent with the carrier substances which can be allowable as drugs. However, it needs to be not restricted in the manner which is demonstrated in this invention. These compositions are dependent on routes and/or planning of administration.
When the acid addition salts or the compounds which is shown in general formula (1-a), (1-b), (2), (3-a) and (3-b) are used as drug above-mentioned, those can be administered orally or non-orally as medicament compositions such as powders, granules, tablets, capsules, injection solutions by suitably mixing with adequate components such as carrier substances, excipients or attenuants which are allowable pharmaceutically. Also, an effect of the compounds can be expected by manner of vapor.
When the compound which is shown in chemical formula (1-a), (1-b), (2), (3-a) and (3-b) of this invention is used by oral route, several types of tablets, capsules, powder materials, granular agents and liquid agents are available. When the compound is administered through the non-oral route, those are used in the form of disinfected fluid. When the compounds are used as types above-mentioned, the carrier substances with nontoxic solids or fluids include in a composition.
As an example of solid carriers, capsules made by usual gelatin is used. Moreover, effective ingredients are utilized with subsidiary substances or by tabulating, granulating and/or powder packaging without subsidiary substances. The following substances are used as the excipients; gelatin, lactose, sugars such as glucose, cone, wheat, rice, starches such as corn starch, fatty acids such as stearic acid, fat bases such as calcium stearic acid and magnesium stearic acid, talc, vegetable oil, alcohol such as stearylalcohol and benzyl alcohol, gum, polyethylene alkylene glycol and so on.
These capsule, tablet, granule and powder are generally 0.1-80 weight % and contains effective ingredient of 0.1-60 weight %. Liquid carriers such as water, physiological saline, sugar solution, dextrose solution, ethylene glycol, propylene glycol, glycols such as polyethylene glycol, polyoxyethylene sorbitan monoolate are desirable.
When it is administered non-orally by the manner of intramuscular injection, intravenous injection or hypodermic injection, the compounds provided in general formula (1-a), (1-b), (2), (3-a) and (3-b) are used as the germ-free solution which is added other solutes such as minerals or glucose in order to make the isotonic solution. Appropriate solvents for an injection represent sterilizing water, solution of lidocaine hydrochloride (for intramuscular injection), physiological saline, glucose solution, any kind of fluids for an intravenous injection, electrolyte solution (for intravenous injection) and so on. When those solutions for the injection are used, usual dosage is 0.01-20 weight % and is desirable at 0.05-5 weight %.
In the case of liquids for oral administration, it is better to be used as suspension or syrup with 0.01-20 weight %. A carrier of these liquids is watery excipient such as perfume, syrup and micelle which are available for pharmaceutic manufacturing.
When the compounds in this invention are drug-manufactured by combination with the carriers which is allowable on pharmaceutics, usually known methods and techniques are avairable. Concretely, when ointment, cream agents, emulsions or milky lotions are produced, silver-carried inorganic compounds, drugs and halogen compounds as occasion demands are added at melting and mixing, simultaneously, during and after emulsification resulting in ointments, cream agents or milky lotions. Also, drugs and/or halogen compounds can be added firstly. When the compounds in this invention are used as sterilizing agents and disinfectants for living space, an effect can be obtained by single use or combination with suitable carriers. Concretely, it makes operate directly or indirectly through a room air to solid surface by aspersion, embrocation or evaporation.
Also, a sterilizing effect can be obtained by adding the compounds into water of humidifier and on any part of circulation circuits of air-conditioning device. In addition, when the compounds in this invention composition are used as depolymerization agents, improving agents for surface active substances, reductants, free radical scavengers, desulfurization agents, phase transition agents, improving agents of phase transition, improving agents of microphase separation structure, promoting agents for plasticity and/or elasticity, improving agent for plasticity and/or elasticity, copolymerization agents, copolymerization improving agents, polymerization regulators, improving agents for polymerization adjustment, stabilizers, antioxidants, improving agents for crystallized materials and/or amorphous materials, flexibility promoters and/or improving agents for changing in flexibility, those compounds can effectively control, inhibit and/or generate an objective property of substances by using as a single substance and/or a combination with adequate carriers. When the compounds in this invention are used as modulators or improving agents for fluorescent wavelength and excitation wavelength of pigmentums, coating materials, cosmetic pigments or colorants, improving agents of physical property with low molecule substance, improving agents of function with low molecule substance, improving agents of physical property of macromolecules substance, improving agents of function with macromolecules substance and/or improving agents of physical property with macromolecules composite materials and functional macromolecules composite materials, those compounds can effectively control, inhibit and/or generate an objective property with substances by using as a single substance and/or a combination with adequate carriers. Concretely, an improvement of efficiencies can be planned by selecting a mixing ratio with macromolecules substances, a churning temperature, an adjusting energy quantity such as protons and radio waves and/or transition metals.